S7397 |
Sorafenib
|
Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
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Cell Rep Med, 2024, S2666-3791(24)00201-5
-
J Exp Clin Cancer Res, 2024, 43(1):143
-
Biomed Pharmacother, 2024, 173:116366
|
|
S1040 |
Sorafenib tosylate
|
Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
-
Cell Mol Life Sci, 2024, 81(1):238
-
J Transl Med, 2024, 22(1):593
-
Front Immunol, 2024, 15:1373321
|
|
S7781 |
Sunitinib
|
Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis. |
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Pharmaceuticals (Basel), 2024, 17(1)77
-
Heliyon, 2024, 10(3):e24779
|
|
S1490 |
Ponatinib
|
Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy. |
-
Int J Biol Sci, 2024, 20(9):3412-3425
-
Cell Rep, 2024, 43(3):113932
-
Elife, 2024, 12RP92324
|
|
S1178 |
Regorafenib
|
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
-
Nat Med, 2024, 10.1038/s41591-024-02824-y
-
Nature, 2024, 629(8011):450-457
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
|
|
S1005 |
Axitinib
|
Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. |
-
Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
EMBO Mol Med, 2024, 10.1038/s44321-024-00094-2
|
|
S1042 |
Sunitinib malate
|
Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. |
-
Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
-
Pharmaceuticals (Basel), 2024, 17(1)108
-
Cell Cycle, 2024, 1-13.
|
|
S1029 |
Lenalidomide
|
Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis. |
-
Clin Immunol, 2024, 260:109915
-
Oncogene, 2024, 43(3):155-170
-
Eur J Pharmacol, 2024, 979:176835
|
|
S1119 |
Cabozantinib (XL184)
|
Cabozantinib (XL184) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway. |
-
Front Immunol, 2024, 15:1258475
-
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
-
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
|
|
S1010 |
Nintedanib
|
Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3. |
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Cells, 2024, 13(13)1152
-
Invest Ophthalmol Vis Sci, 2024, 65(2):30
|
|
S1264 |
PD173074
|
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells. |
-
bioRxiv, 2024, 2024.01.23.576717
-
Malignancy Spectrum, 2024, 10.1002/msp2.20
-
JCI Insight, 2023, 8(10)e154729
|
|
S1046 |
Vandetanib
|
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS). |
-
Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
-
Front Pharmacol, 2024, 15:1345070
-
Front Pharmacol, 2024, 15:1345070
|
|
S1164 |
Lenvatinib
|
Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. |
-
Nat Commun, 2024, 15(1):1754
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Redox Biol, 2024, 75:103270
|
|
S4001 |
Cabozantinib malate
|
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
-
Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
-
Cancer Sci, 2023, 114(4):1651-1662
-
Cancer Sci, 2023, 114(4):1651-1662
|
|
S1111 |
Foretinib
|
Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
-
Int J Mol Sci, 2023, 24(1)757
-
Biol Open, 2023, 12(8)bio059994
-
Melanoma Res, 2023, 10.1097/CMR.0000000000000911
|
|
S3012 |
Pazopanib
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. |
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Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Transl Psychiatry, 2024, 14(1):166
-
Cancer Med, 2024, 13(11):e7291
|
|
S1017 |
Cediranib (AZD2171)
|
Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3. |
-
Front Oncol, 2024, 14:1302850
-
Cell Oncol (Dordr), 2023, 46(2):391-407
-
Cell Oncol (Dordr), 2023, 46(2):391-407
|
|
S1035 |
Pazopanib HCl
|
Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. |
-
iScience, 2023, 26(7):107116
-
NPJ Breast Cancer, 2022, 8(1):44
-
J Pers Med, 2022, 12(2)258
|
|
S1018 |
Dovitinib (TKI-258)
|
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. |
-
Sci Rep, 2023, 13(1):20223
-
Sci Adv, 2023, 9(9):eadd2671
-
UFTM, 2023,
|
|
S1101 |
Vatalanib (PTK787) 2HCl
|
Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3. |
-
Environ Health Perspect, 2024, 132(5):57001
-
J Cancer, 2024, 15(9):2448-2459
-
J Exp Clin Cancer Res, 2023, 42(1):79
|
|
S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
-
STAR Protoc, 2024, 5(2):103090
-
J Clin Med, 2023, 12(23)7267
-
J Hematol Oncol, 2022, 15(1):109
|
|
S1207 |
Tivozanib
|
Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. |
-
Nat Commun, 2024, 15(1):4758
-
Nat Commun, 2024, 15(1):4758
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
|
|
A2006 |
Bevacizumab (anti-VEGF)
|
Bevacizumab (anti-VEGF, Avastin) is a humanized anti-VEGF monoclonal antibody which binds to and neutralizes all human VEGF-A isoforms and bioactive proteolytic fragments, MW:149 KD. |
-
Nat Commun, 2024, 15(1):1359
-
Front Immunol, 2024, 15:1273280
-
Front Oncol, 2024, 14:1302850
|
|
S8401 |
Erdafitinib
|
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
-
J Clin Invest, 2024, 134(2)e169241
-
Adv Sci (Weinh), 2024, 11(16):e2303379
-
Mol Oncol, 2024, 10.1002/1878-0261.13684
|
|
S1003 |
Linifanib (ABT-869)
|
Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3. |
-
Cell Death Discov, 2023, 9(1):57
-
Cell Death Discov, 2023, 9(1):57
-
Cancer Cell, 2022, S1535-6108(22)00312-9
|
|
S8726 |
Anlotinib (AL3818) dihydrochloride
|
Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation. |
-
Cell Rep Med, 2024, 5(2):101416
-
Braz J Med Biol Res, 2024, 57:e13152
-
Cancer Cell Int, 2023, 23(1):309
|
|
S7765 |
Dovitinib (TKI258) Lactate monohydrate
|
Dovitinib (TKI258) Lactate monohydrate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
|
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Mol Cell, 2021, S1097-2765(21)00507-4
-
Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
-
Cancer Res, 2021, canres.1780.2020
|
|
S5240 |
Lenvatinib Mesylate
|
Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. |
-
Nat Commun, 2024, 15(1):1754
-
J Hepatocell Carcinoma, 2023, 10:697-712
-
Discov Oncol, 2023, 14(1):26
|
|
S2161 |
RAF265 (CHIR-265)
|
RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2. |
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Cancer Cell, 2022, S1535-6108(22)00312-9
-
iScience, 2022, 25(10):105182
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Cancers (Basel), 2022, 14(6)1575
|
|
S2842 |
SAR131675
|
SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc. |
-
Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
-
Theranostics, 2024, 14(5):1886-1908
-
Cell Rep, 2023, 42(5):112489
|
|
S5248 |
Apatinib
|
Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis. |
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Cancer Cell, 2024, 42(4):535-551.e8
-
Sci Rep, 2024, 14(1):879
-
Adv Sci (Weinh), 2023, 10(23):e2300898
|
|
S2221 |
Apatinib (YN968D1) mesylate
|
Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis. |
-
Clin Respir J, 2024, 18(2):e13738
-
J Pers Med, 2022, 12(2)258
-
Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S4947 |
Regorafenib Hydrochloride
|
Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
-
Cancers (Basel), 2023, 15(18)4477
-
Cancers (Basel), 2023, 15(18)4477
-
J Clin Med, 2023, 12(23)7267
|
|
S1363 |
Ki8751
|
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. |
-
Nat Commun, 2024, 15(1):2539
-
Drug Des Devel Ther, 2023, 17:1567-1582
-
Transl Oncol, 2022, 25:101516
|
|
S2896 |
ZM 323881 HCl
|
ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. |
-
Stem Cells Transl Med, 2023, szad049
-
Stem Cells Transl Med, 2023, 12(10):676-688
-
iScience, 2023, 26(9):107548
|
|
S2845 |
Semaxanib (SU5416)
|
Semaxanib (SU5416, semaxinib) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3. |
-
Nat Commun, 2024, 15(1):4758
-
Nat Commun, 2024, 15(1):4758
-
Nat Commun, 2024, 15(1):4758
|
|
S7057 |
LY2874455
|
LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
|
-
Cancer Discov, 2023, 13(9):1998-2011
-
Cancer Discov, 2023, 13(9):1998-2011
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Cancer Discov, 2023, 13(9):1998-2011
|
|
S5234 |
Nintedanib Ethanesulfonate Salt
|
Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. |
-
Am J Cancer Res, 2023, 13(2):355-378
-
Theranostics, 2022, 12(2):747-766
-
EMBO Mol Med, 2022, 14(3):e15295
|
|
S7667 |
SU5402
|
SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
|
-
Regen Ther, 2024, 25:229-237
-
Dis Model Mech, 2023, 16(7)dmm050066
-
J Vis Exp, 2023, (202).
|
|
S1486 |
AEE788 (NVP-AEE788)
|
AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. |
-
Cell Rep Med, 2022, 3(1):100492
-
Genome Med, 2020, 18;12(1):17
-
Oncotarget, 2019, 10(68):7185-7197
|
|
S5242 |
Cediranib Maleate
|
Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM. |
-
J Exp Clin Cancer Res, 2024, 43(1):56
-
Cell Oncol (Dordr), 2022, 45(4):601-619
-
Mol Cancer Ther, 2022, 21(6):1030-1043
|
|
S1032 |
Motesanib Diphosphate (AMG-706)
|
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. |
-
Front Cell Dev Biol, 2022, 10:836179
-
J Pharm Sci, 2022, 111(8):2180-2190
-
Drug Metab Dispos, 2021, 49(1):53-61
|
|
S1361 |
MGCD-265 analog
|
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2. |
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Cell Rep Med, 2022, 3(1):100492
-
Protein Cell, 2019, 10(3):161-177
|
|
S1084 |
Brivanib (BMS-540215)
|
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3. |
-
Stem Cells Transl Med, 2023, szad049
-
Stem Cells Transl Med, 2023, 12(10):676-688
-
iScience, 2023, 26(9):107548
|
|
S2897 |
ZM 306416
|
ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM. |
-
Nat Commun, 2024, 15(1):4758
-
Int J Mol Sci, 2024, 25(5)2956
-
J Pharmacol Sci, 2023, 151(4):177-186
|
|
S5793 |
Motesanib (AMG-706)
|
Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively. |
-
Signal Transduct Target Ther, 2022, 7(1):147
-
Front Cell Dev Biol, 2022, 10:836179
-
J Pharm Sci, 2022, 111(8):2180-2190
|
|
S1181 |
ENMD-2076
|
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. |
-
Cell, 2021, 184(2):334-351.e20
-
Sci Adv, 2021, 7(4)eabd7851
-
J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S1171 |
CYC116
|
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1. |
-
Sci Rep, 2024, 14(1):4303
-
Cell Chem Biol, 2023, 30(8):987-998.e24
-
Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
|
|
S2859 |
Golvatinib (E7050)
|
Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2. |
-
Int J Mol Sci, 2023, 24(11)9606
-
Int J Mol Sci, 2022, 23(23)14884
-
Cancer Sci, 2020, 111(10):3813-3823
|
|
S4686 |
Vitamin E
|
Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription. |
-
Signal Transduct Target Ther, 2024, 9(1):109
-
Signal Transduct Target Ther, 2024, 9(1):109
-
medRxiv, 2023, 10.1101/2023.12.01.23299102
|
|
S1220 |
OSI-930
|
OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. |
-
Nat Commun, 2024, 15(1):4739
-
Cell Rep, 2019, 28(9):2331-2344
-
Nat Biomed Eng, 2018, 2(8):578-588
|
|
S2622 |
PP121
|
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. |
-
Life Sci Alliance, 2021, 4(2)e202000882
-
PLoS One, 2016, 11(10):e0164895
-
PLoS One, 2016, 11(10):e0164895
|
|
S1557 |
KRN 633
|
KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell. |
-
Aust Dent J, 2020, 10.1111/adj.12752
-
J Med Invest, 2017, 64(3.4):262-265
-
Oncotarget, 2016, 7(5):5985-99
|
|
S2231 |
Telatinib
|
Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. |
-
Sci Adv, 2022, 8(6):eabg9455
-
Leiden University Scholarly Publications, 2020, N/A
-
Cell Stem Cell, 2019, 24(4):654-669
|
|
S5667 |
Fruquintinib
|
Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases. |
-
EMBO J, 2024, 43(8):1519-1544
-
Cancer Commun (Lond), 2023, 10.1002/cac2.12411
-
Dev Cell, 2022, 57(12):1466-1481.e6
|
|
S8573 |
Sitravatinib (MGCD516)
|
Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. |
-
JCI Insight, 2022, e148717
-
Cancers (Basel), 2021, 13(21)5474
-
Cancers (Basel), 2020, 12(1)
|
|
S7258 |
SKLB1002
|
SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM. |
-
Sci Adv, 2024, 10(20):eadl0633
-
Sci Adv, 2024, 10(20):eadl0633
-
Dis Model Mech, 2023, 16(5)dmm049571
|
|
S7003 |
AZD2932
|
AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
|
-
Cancer Res, 2020, canres.1992.2020
-
Molecules, 2020, 8;25(9) pii: E2220
-
Development, 2016, 143(23):4394-4404
|
|
S2366 |
Taxifolin (Dihydroquercetin)
|
Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on. |
-
Sci Rep, 2020, 10(1):17311
-
J Med Virol, 2019, 91(8):1440-1447
-
Cytotechnology, 2016, 68(4):1633-40
|
|
S1138 |
Brivanib Alaninate (BMS-582664)
|
Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM. |
-
Int J Oncol, 2014, 44(3):959-69
-
Assay Drug Dev Technol, 2014, 12(9-10):514-26
|
|
S8189 |
BAW2881 (NVP-BAW2881)
|
BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. |
-
JCI Insight, 2021, 143285
-
J Cell Biochem, 2019, 120(4):5583-5596
|
|
S0504 |
SU14813
|
SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. |
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Adv Sci (Weinh), 2021, e2101848
|
|
S6535 |
SU1498
|
SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells. |
-
Cell Metab, 2020, 5;31(5):892-908 e11
-
Biol Open, 2018,
|
|
S8721 |
PDGFR inhibitor 1
|
PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
-
Elife, 2023, 12e79840
-
Elife, 2023, 12e79840
-
Oncogene, 2022, 41(20):2860-2872
|
|
S0278 |
SU5614
|
SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis. |
-
Adv Sci (Weinh), 2021, e2101848
-
Front Cell Dev Biol, 2021, 9:797047
|
|
S6526 |
SKLB 610
|
SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR. |
-
Biomed Pharmacother, 2022, 149:112922
-
Int J Mol Sci, 2022, 23(14)7853
|
|
S6412 |
Altiratinib
|
Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM. |
-
Theranostics, 2021, 11(20):9918-9936
-
Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
|
|
S6514 |
SU5408
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM. |
-
Transl Oncol, 2022, 25:101516
-
J Dent Sci, 2022, 17(4):1471-1479
|
|
S2201 |
BMS-794833
|
BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1. |
-
Cancer Res, 2021, canres.1428.2021
|
|
S0290 |
SU5204
|
SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively. |
-
Front Pharmacol, 2021, 12:804327
|
|
A2003 |
Ramucirumab (anti-VEGFR2)
|
Ramucirumab is a monoclonal antibody of the IgG1 class that binds to VEGF-R2 and prevents its activation. The IC50 value for blocking KDR binding to VEGF is 0.8 nM for ramucirumab, MW: 143.6 KD. |
-
Cancer Immunol Immunother, 2024, 73(10):190
-
Int J Mol Sci, 2024,
-
Int J Mol Sci, 2024, 25(3)1769
|
|
S0487 |
Sulfatinib
|
Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
-
Front Oncol, 2023, 13:1158857
|
|
S2018 |
ENMD-2076 L-(+)-Tartaric acid
|
ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2. |
|
|
S6520 |
WHI-P180
|
WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively. |
|
|
S6543 |
ZD-4190
|
ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively. |
|
|
S7688 |
Ki20227
|
Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. |
-
Cancer Immunol Immunother, 2024, 73(5):76
-
Cancer Immunol Immunother, 2024, 73(5):76
|
|
S5272 |
Toceranib phosphate
|
Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. |
-
Front Vet Sci, 2024, 11:1392728
|
|
S8188 |
BFH772
|
BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM. |
|
|
S0291 |
SU5208
|
SU5208(3-[(Thien-2-yl)methylene]-2-indolinone) is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2). |
|
|
A2126New |
Anti-mouse VEGFR-2-InVivo
|
Anti-mouse VEGFR-2-InVivo (Clone: DC101) monoclonal antibody reacts with mouse VEGFR-2 (vascular endothelial growth factor receptor 2) also known as CD309, KDR, and Flk-1 and inhibit VEGFR-2 signaling in vivo. VEGFR-2 plays a key role in vascular development and permeability. |
|
|
E2397 |
hVEGF-IN-1
|
hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression. |
|
|
S8882 |
ODM-203
|
ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively. |
|
|
S0763 |
Tyrphostin AG1433
|
Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. |
|
|
S0765 |
MAZ51
|
MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines. |
|
|
E0499 |
4SC-203
|
4SC-203 (SC71710) is a multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
|
|
|
E2656 |
R1530
|
R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor for the treatment of solid tumors, which can inhibit vascular endothelial growth factor receptor 2 (VEGFR2) and fibroblast growth factor receptors 1 (FGFR1) with IC50s of 10 nM and 28 nM, respectively. |
|
|
S9621 |
Donafenib (Sorafenib D3)
|
Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. |
|
|
E1078 |
Emvododstat (PTC299)
|
Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM. |
|
|
S2211 |
AG-13958
|
AG-13958 (AG-013958), a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD). |
|
|
S5607 |
4,4'-Bis(4-aminophenoxy)biphenyl
|
4,4'-Bis(4-aminophenoxy)biphenyl is a monomer for polyimide production. |
|
|
S7647 |
Lucitanib (E3810) hydrochloride
|
Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. |
-
Sci Rep, 2023, 13(1):20223
|
|
E0616 |
Chiauranib
|
Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |
|
|
S6870 |
Ningetinib
|
Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity. |
|
|
S6843 |
Vorolanib
|
Vorolanib (X-82,CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. |
|
|
S6764 |
Pamufetinib (TAS-115)
|
Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively. |
|
|
S6939 |
Nastorazepide
|
Nastorazepide (Z-360), a cholecystokinin-2/gastrin receptor (CCK2/gastrin receptor) antagonist, combines with gemcitabine prolonged survival and reduces gemcitabine-induced vascular endothelial growth factor (VEGF) expression in a pancreatic carcinoma orthotopic xenograft mouse. |
|
|
E3379 |
Cassia seed Extract
|
Cassia seed Extract is extracted from seed of Cassia toraLinn, has the potential to influence varieties of biological processes and pathways, including positive regulation of smooth muscle cell proliferation, inflammatory response, tumor necrosis factor (TNF) signaling pathway, vascular endothelial growth factor (VEGF) signaling pathway and arachidonic acid (ARA) metabolism. |
|
|
S0377 |
CS-2660 (JNJ-38158471)
|
CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
|
|
E0534 |
WAY-340935
|
WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein. |
|
|
S9402 |
(20R)-Protopanaxadiol
|
(20R)-Protopanaxadiol, isolated from the roots of Panax ginseng, has protective effect on myocardial ischemia. |
|
|
E3414 |
Semen litchi Extract
|
Semen litchi Extract is extracted from Litchi chinensis, which has an anti-hepatoma effect and inhibits angiogenesis by targeting VEGFR in hepatocellular carcinoma. |
|
|
E0207 |
Chebulinic acid
|
Chebulinic acid, a phenolic compound isolated from Terminalia chebula fruit, is a novel Influenza viral neuraminidase inhibitor. Chebulinic acid is a antiangiogenic agent through inhibiting the actions of VEGF. Chebulinic acid shows antitumour activity.
|
|
|
E3774 |
Chlorella Pyrenoidosa Extract
|
Chlorella Pyrenoidosa Extract is extracted from Chlorella pyrenoidosa, which exerts a significant antiangiogenic activity was observed against VEGF-induced neovascularization and antiproliferative activity. |
|
|
S6808 |
SU5205
|
SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM. |
|
|
S6809 |
SU5214
|
SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively. |
|
|
E1435New |
Tinengotinib
|
Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
|
|
E0142 |
XL092
|
XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
|
|
|
A2126New |
Anti-mouse VEGFR-2-InVivo
|
Anti-mouse VEGFR-2-InVivo (Clone: DC101) monoclonal antibody reacts with mouse VEGFR-2 (vascular endothelial growth factor receptor 2) also known as CD309, KDR, and Flk-1 and inhibit VEGFR-2 signaling in vivo. VEGFR-2 plays a key role in vascular development and permeability. |
|
|
S7397 |
Sorafenib
|
Sorafenib is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- J Exp Clin Cancer Res, 2024, 43(1):143
- Biomed Pharmacother, 2024, 173:116366
|
|
S1040 |
Sorafenib tosylate
|
Sorafenib tosylate is a multikinase inhibitor of Raf-1 and B-Raf with IC50 of 6 nM and 22 nM in cell-free assays, respectively. Sorafenib Tosylate inhibits VEGFR-2, VEGFR-3, PDGFR-β, Flt-3 and c-KIT with IC50 of 90 nM, 20 nM, 57 nM, 59 nM and 68 nM, respectively. Sorafenib Tosylate induces autophagy and apoptosis and activates ferroptosis with anti-tumor activity. |
- Cell Mol Life Sci, 2024, 81(1):238
- J Transl Med, 2024, 22(1):593
- Front Immunol, 2024, 15:1373321
|
|
S7781 |
Sunitinib
|
Sunitinib is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM, and also inhibits c-Kit. Sunitinib is also a dose-dependent inhibitor of the autophosphorylation activity of IRE1α. Sunitinib induces autophagy and apoptosis. |
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- Pharmaceuticals (Basel), 2024, 17(1)77
- Heliyon, 2024, 10(3):e24779
|
|
S1490 |
Ponatinib
|
Ponatinib is a novel, potent multi-target inhibitor of Abl, PDGFRα, VEGFR2, FGFR1 and Src with IC50 of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM and 5.4 nM in cell-free assays, respectively. Ponatinib (AP24534) inhibits autophagy. |
- Int J Biol Sci, 2024, 20(9):3412-3425
- Cell Rep, 2024, 43(3):113932
- Elife, 2024, 12RP92324
|
|
S1178 |
Regorafenib
|
Regorafenib is a multi-target inhibitor for VEGFR1, VEGFR2, VEGFR3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM/4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM in cell-free assays, respectively. Regorafenib induces autophagy. |
- Nat Med, 2024, 10.1038/s41591-024-02824-y
- Nature, 2024, 629(8011):450-457
- Cell Rep Med, 2024, S2666-3791(24)00201-5
|
|
S1005 |
Axitinib
|
Axitinib is a multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFRβ and c-Kit with IC50 of 0.1 nM, 0.2 nM, 0.1-0.3 nM, 1.6 nM and 1.7 nM in Porcine aorta endothelial cells, respectively. |
- Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- EMBO Mol Med, 2024, 10.1038/s44321-024-00094-2
|
|
S1042 |
Sunitinib malate
|
Sunitinib malate is a multi-targeted RTK inhibitor targeting VEGFR2 (Flk-1) and PDGFRβ with IC50 of 80 nM and 2 nM in cell-free assays, and also inhibits c-Kit. Sunitinib Malate effectively inhibits autophosphorylation of Ire1α. Sunitinib Malate increases both death receptor and mitochondrial-dependent apoptosis. |
- Cell Oncol (Dordr), 2024, 10.1007/s13402-024-00939-5
- Pharmaceuticals (Basel), 2024, 17(1)108
- Cell Cycle, 2024, 1-13.
|
|
S1029 |
Lenalidomide
|
Lenalidomide is a TNF-α secretion inhibitor with IC50 of 13 nM in PBMCs. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide promotes cleaved caspase-3 expression and inhibit VEGF expression and induces apoptosis. |
- Clin Immunol, 2024, 260:109915
- Oncogene, 2024, 43(3):155-170
- Eur J Pharmacol, 2024, 979:176835
|
|
S1119 |
Cabozantinib (XL184)
|
Cabozantinib (XL184) is a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway. |
- Front Immunol, 2024, 15:1258475
- Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
- Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
|
|
S1010 |
Nintedanib
|
Nintedanib is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM in cell-free assays. Phase 3. |
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- Cells, 2024, 13(13)1152
- Invest Ophthalmol Vis Sci, 2024, 65(2):30
|
|
S1264 |
PD173074
|
PD173074 is a potent FGFR1 inhibitor with IC50 of ~25 nM and also inhibits VEGFR2 with IC50 of 100-200 nM in cell-free assays, ~1000-fold selective for FGFR1 than PDGFR and c-Src. PD173074 reduces proliferation and promotes apoptosis in gastric cancer cells. |
- bioRxiv, 2024, 2024.01.23.576717
- Malignancy Spectrum, 2024, 10.1002/msp2.20
- JCI Insight, 2023, 8(10)e154729
|
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S1046 |
Vandetanib
|
Vandetanib is a potent inhibitor of VEGFR2 with IC50 of 40 nM in a cell-free assay. It also inhibits VEGFR3 and EGFR with IC50 of 110 nM and 500 nM, respectively. Not sensitive to PDGFRβ, Flt1, Tie-2 and FGFR1 with IC50 of 1.1-3.6 μM. No activity against MEK, CDK2, c-Kit, erbB2, FAK, PDK1, Akt and IGF-1R with IC50 above 10 μM. Vandetanib (ZD6474) increases apoptosis and induces autophagy by increasing the level of reactive oxygen species (ROS). |
- Biochim Biophys Acta Mol Basis Dis, 2024, 1870(6):167249
- Front Pharmacol, 2024, 15:1345070
- Front Pharmacol, 2024, 15:1345070
|
|
S1164 |
Lenvatinib
|
Lenvatinib is a multi-target inhibitor, mostly for VEGFR2(KDR)/VEGFR3(Flt-4) with IC50 of 4 nM/5.2 nM, less potent against VEGFR1/Flt-1, ~10-fold more selective for VEGFR2/3 against FGFR1, PDGFRα/β in cell-free assays. Lenvatinib (E7080) also inhibits FGFR1-4, PDGFR, Kit (c-Kit), RET (c-RET), and shows potent antitumor activities. Phase 3. |
- Nat Commun, 2024, 15(1):1754
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- Redox Biol, 2024, 75:103270
|
|
S4001 |
Cabozantinib malate
|
Cabozantinib malate (XL184) is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret (c-Ret), Kit (c-Kit), Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM in cell-free assays, respectively. Cabozantinib malate (XL184) induces apoptosis. |
- Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
- Cancer Sci, 2023, 114(4):1651-1662
- Cancer Sci, 2023, 114(4):1651-1662
|
|
S1111 |
Foretinib
|
Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met (c-Met) and KDR with IC50 of 0.4 nM and 0.9 nM in cell-free assays. Less potent against Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
- Int J Mol Sci, 2023, 24(1)757
- Biol Open, 2023, 12(8)bio059994
- Melanoma Res, 2023, 10.1097/CMR.0000000000000911
|
|
S3012 |
Pazopanib
|
Pazopanib (GW786034) is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms/CSF1R with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces cathepsin B activation and autophagy. |
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- Transl Psychiatry, 2024, 14(1):166
- Cancer Med, 2024, 13(11):e7291
|
|
S1017 |
Cediranib (AZD2171)
|
Cediranib (AZD2171, NSC-732208) is a highly potent VEGFR(KDR) inhibitor with IC50 of <1 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM, similar activity against c-Kit and PDGFRβ, 36-, 110-fold and >1000-fold selective more for VEGFR than PDGFR-α, CSF-1R and Flt3 in HUVEC cells. Cediranib (AZD2171) induces autophagic vacuole accumulation. Phase 3. |
- Front Oncol, 2024, 14:1302850
- Cell Oncol (Dordr), 2023, 46(2):391-407
- Cell Oncol (Dordr), 2023, 46(2):391-407
|
|
S1035 |
Pazopanib HCl
|
Pazopanib HCl is a novel multi-target inhibitor of VEGFR1, VEGFR2, VEGFR3, PDGFR, FGFR, c-Kit and c-Fms with IC50 of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II cell death. |
- iScience, 2023, 26(7):107116
- NPJ Breast Cancer, 2022, 8(1):44
- J Pers Med, 2022, 12(2)258
|
|
S1018 |
Dovitinib (TKI-258)
|
Dovitinib (TKI258, CHIR258) is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGF-1R and HER2 in cell-free assays. Phase 4. |
- Sci Rep, 2023, 13(1):20223
- Sci Adv, 2023, 9(9):eadd2671
- UFTM, 2023,
|
|
S1101 |
Vatalanib (PTK787) 2HCl
|
Vatalanib 2HCl (PTK787, ZK 222584, cpg-79787) is an inhibitor of VEGFR2/KDR with IC50 of 37 nM in a cell-free assay, less potent against VEGFR1/Flt-1, 18-fold against VEGFR3/Flt-4. Phase 3. |
- Environ Health Perspect, 2024, 132(5):57001
- J Cancer, 2024, 15(9):2448-2459
- J Exp Clin Cancer Res, 2023, 42(1):79
|
|
S5077 |
Regorafenib (BAY-734506) Monohydrate
|
Regorafenib (BAY-734506, Fluoro-sorafenib, Resihance, Stivarga, regorafaenib monohydrate) Monohydrate is a novel oral multikinase inhibitor with IC50 values of 13, 4.2, 46, 22, 7, 1.5, 2.5, 28, 19 nM for VEGFR1, murine VEGFR2, murine VEGFR3, PDGFR-β, Kit (c-Kit), RET (c-RET), RAF-1, B-RAF and B-RAF(V600E) respectively. |
- STAR Protoc, 2024, 5(2):103090
- J Clin Med, 2023, 12(23)7267
- J Hematol Oncol, 2022, 15(1):109
|
|
S1207 |
Tivozanib
|
Tivozanib is a potent and selective VEGFR inhibitor for VEGFR1/2/3 with IC50 of 30 nM/6.5 nM/15 nM, and also inhibits PDGFR and c-Kit, low activity observed against FGFR-1, Flt3, c-Met, EGFR and IGF-1R. Phase 3. |
- Nat Commun, 2024, 15(1):4758
- Nat Commun, 2024, 15(1):4758
- Cell Rep Med, 2024, S2666-3791(24)00201-5
|
|
S8401 |
Erdafitinib
|
Erdafitinib is a potent and selective orally bioavailable, pan fibroblast growth factor receptor (FGFR) inhibitor with potential antineoplastic activity. Erdafitinib also binds to RET (c-RET), CSF-1R, PDGFR-α/PDGFR-β, FLT4, Kit (c-Kit) and VEGFR-2 and induces cellular apoptosis. |
- J Clin Invest, 2024, 134(2)e169241
- Adv Sci (Weinh), 2024, 11(16):e2303379
- Mol Oncol, 2024, 10.1002/1878-0261.13684
|
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S1003 |
Linifanib (ABT-869)
|
Linifanib (ABT-869, AL39324, RG3635) is a novel, potent ATP-competitive VEGFR/PDGFR inhibitor for KDR, CSF-1R, Flt-1/3 and PDGFRβ with IC50 of 4 nM, 3 nM, 3 nM/4 nM and 66 nM respectively, mostly effective in mutant kinase-dependent cancer cells (i.e. FLT3). Linifanib (ABT-869) induces autophagy and apoptosis. Phase 3. |
- Cell Death Discov, 2023, 9(1):57
- Cell Death Discov, 2023, 9(1):57
- Cancer Cell, 2022, S1535-6108(22)00312-9
|
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S8726 |
Anlotinib (AL3818) dihydrochloride
|
Anlotinib (AL3818) is a highly potent and selective VEGFR2 inhibitor with IC50 less than 1 nM. It has broad-spectrum antitumor potential in clinical trials. Please use saline solution rather than PBS for dilutions. PBS may cause precipitation. |
- Cell Rep Med, 2024, 5(2):101416
- Braz J Med Biol Res, 2024, 57:e13152
- Cancer Cell Int, 2023, 23(1):309
|
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S7765 |
Dovitinib (TKI258) Lactate monohydrate
|
Dovitinib (TKI258) Lactate monohydrate is the Lactate of Dovitinib, which is a multitargeted RTK inhibitor, mostly for class III (FLT3/c-Kit) with IC50 of 1 nM/2 nM, also potent to class IV (FGFR1/3) and class V (VEGFR1-4) RTKs with IC50 of 8-13 nM, less potent to InsR, EGFR, c-Met, EphA2, Tie2, IGFR1 and HER2. Phase 4.
|
- Mol Cell, 2021, S1097-2765(21)00507-4
- Acta Neuropathol, 2021, 10.1007/s00401-021-02327-x
- Cancer Res, 2021, canres.1780.2020
|
|
S5240 |
Lenvatinib Mesylate
|
Lenvatinib Mesylate is a synthetic, orally available tyrosine kinase inhibitor that inhibits vascular endothelial growth factor receptor (VEGFR1-3), fibroblast growth factor receptor (FGFR1-4), platelet-derived growth factor receptor α (PDGFRα), stem cell factor receptor (Kit (c-Kit)), and rearranged during transfection (RET (c-RET)). Lenvatinib Mesylate has potential antineoplastic activity. |
- Nat Commun, 2024, 15(1):1754
- J Hepatocell Carcinoma, 2023, 10:697-712
- Discov Oncol, 2023, 14(1):26
|
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S2161 |
RAF265 (CHIR-265)
|
RAF265 (CHIR-265) is a potent selective inhibitor of C-Raf/B-Raf/B-Raf V600E with IC50 of 3-60 nM, and exhibits potent inhibition on VEGFR2 phosphorylation with EC50 of 30 nM in cell-free assays. RAF265 (CHIR-265) induces cell cycle arrest and apoptosis. Phase 2. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- iScience, 2022, 25(10):105182
- Cancers (Basel), 2022, 14(6)1575
|
|
S2842 |
SAR131675
|
SAR131675 is a VEGFR3 inhibitor with IC50/Ki of 23 nM/12 nM in cell-free assays, about 50- and 10-fold more selective for VEGFR3 than VEGFR1/2, little activity against Akt1, CDKs, PLK1, EGFR, IGF-1R, c-Met, Flt2 etc. |
- Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
- Theranostics, 2024, 14(5):1886-1908
- Cell Rep, 2023, 42(5):112489
|
|
S5248 |
Apatinib
|
Apatinib (Rivoceranib, YN968D1) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib induces both autophagy and apoptosis. |
- Cancer Cell, 2024, 42(4):535-551.e8
- Sci Rep, 2024, 14(1):879
- Adv Sci (Weinh), 2023, 10(23):e2300898
|
|
S2221 |
Apatinib (YN968D1) mesylate
|
Apatinib mesylate (YN968D1, Rivoceranib) is a potent inhibitor of the VEGF signaling pathway with IC50 values of 1 nM, 13 nM, 429 nM and 530 nM for VEGFR-2, Ret (c-Ret), c-Kit and c-Src, respectively. Apatinib mesylate induces both autophagy and apoptosis. |
- Clin Respir J, 2024, 18(2):e13738
- J Pers Med, 2022, 12(2)258
- Hum Cell, 2022, 10.1007/s13577-022-00671-y
|
|
S4947 |
Regorafenib Hydrochloride
|
Regorafenib (Stivarga, BAY 73-4506) Hydrochloride is a multi-target inhibitor for VEGFR1, Murine VEGFR2/3, PDGFRβ, Kit (c-Kit), RET (c-RET) and Raf-1 with IC50 of 13 nM, 4.2 nM/46 nM, 22 nM, 7 nM, 1.5 nM and 2.5 nM, respectively. |
- Cancers (Basel), 2023, 15(18)4477
- Cancers (Basel), 2023, 15(18)4477
- J Clin Med, 2023, 12(23)7267
|
|
S1363 |
Ki8751
|
Ki8751 is a potent and selective inhibitor of VEGFR2 with IC50 of 0.9 nM, >40-fold selective for VEGFR2 than c-Kit, PDGFRα and FGFR-2, little activity to EGFR, HGFR and InsR. |
- Nat Commun, 2024, 15(1):2539
- Drug Des Devel Ther, 2023, 17:1567-1582
- Transl Oncol, 2022, 25:101516
|
|
S2896 |
ZM 323881 HCl
|
ZM 323881 is a potent and selective VEGFR2 inhibitor with IC50 of <2 nM, almost no activity on VEGFR1, PDGFRβ, FGFR1, EGFR and ErbB2. |
- Stem Cells Transl Med, 2023, szad049
- Stem Cells Transl Med, 2023, 12(10):676-688
- iScience, 2023, 26(9):107548
|
|
S2845 |
Semaxanib (SU5416)
|
Semaxanib (SU5416, semaxinib) is a potent and selective VEGFR(Flk-1/KDR) inhibitor with IC50 of 1.23 μM, 20-fold more selective for VEGFR than PDGFRβ, lack of activity against EGFR, InsR and FGFR. Phase 3. |
- Nat Commun, 2024, 15(1):4758
- Nat Commun, 2024, 15(1):4758
- Nat Commun, 2024, 15(1):4758
|
|
S7057 |
LY2874455
|
LY2874455 is a pan-FGFR inhibitor with IC50 of 2.8 nM, 2.6 nM, 6.4 nM, and 6 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively, and also inhibits VEGFR2 activity with IC50 of 7 nM. Phase 1.
|
- Cancer Discov, 2023, 13(9):1998-2011
- Cancer Discov, 2023, 13(9):1998-2011
- Cancer Discov, 2023, 13(9):1998-2011
|
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S5234 |
Nintedanib Ethanesulfonate Salt
|
Nintedanib (Intedanib, BIBF 1120) is a small molecule tyrosine-kinase inhibitor with IC50 of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β, respectively. |
- Am J Cancer Res, 2023, 13(2):355-378
- Theranostics, 2022, 12(2):747-766
- EMBO Mol Med, 2022, 14(3):e15295
|
|
S7667 |
SU5402
|
SU5402 is a potent multi-targeted receptor tyrosine kinase inhibitor with IC50 of 20 nM, 30 nM, and 510 nM for VEGFR2, FGFR1, and PDGF-Rβ, respectively.
|
- Regen Ther, 2024, 25:229-237
- Dis Model Mech, 2023, 16(7)dmm050066
- J Vis Exp, 2023, (202).
|
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S1486 |
AEE788 (NVP-AEE788)
|
AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. |
- Cell Rep Med, 2022, 3(1):100492
- Genome Med, 2020, 18;12(1):17
- Oncotarget, 2019, 10(68):7185-7197
|
|
S5242 |
Cediranib Maleate
|
Cediranib Maleate (AZD2171) is the maleate salt of Cediranib, which is a potent inhibitor of VEGFR with IC50 of <1 nM and also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM. |
- J Exp Clin Cancer Res, 2024, 43(1):56
- Cell Oncol (Dordr), 2022, 45(4):601-619
- Mol Cancer Ther, 2022, 21(6):1030-1043
|
|
S1032 |
Motesanib Diphosphate (AMG-706)
|
Motesanib Diphosphate (AMG-706) is a potent ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 2 nM/3 nM/6 nM, respectively; similar activity against Kit (c-Kit), ~10-fold more selective for VEGFR than PDGFR and Ret. Phase 3. |
- Front Cell Dev Biol, 2022, 10:836179
- J Pharm Sci, 2022, 111(8):2180-2190
- Drug Metab Dispos, 2021, 49(1):53-61
|
|
S1361 |
MGCD-265 analog
|
MGCD-265 is a potent, multi-target and ATP-competitive inhibitor of c-Met and VEGFR1/2/3 with IC50 of 1 nM, 3 nM/3 nM/4 nM, respectively; also inhibits Ron and Tie2. Phase 1/2. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Cell Rep Med, 2022, 3(1):100492
- Protein Cell, 2019, 10(3):161-177
|
|
S1084 |
Brivanib (BMS-540215)
|
Brivanib is an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM, moderate potency against VEGFR-1 and FGFR-1, but >240-fold against PDGFR-β. Phase 3. |
- Stem Cells Transl Med, 2023, szad049
- Stem Cells Transl Med, 2023, 12(10):676-688
- iScience, 2023, 26(9):107548
|
|
S2897 |
ZM 306416
|
ZM 306416 (CB 676475) is a VEGFR (Flt and KDR) inhibitor for VEGFR1 with IC50 of 0.33 μM, but also found to inhibit EGFR with IC50 of <10 nM. |
- Nat Commun, 2024, 15(1):4758
- Int J Mol Sci, 2024, 25(5)2956
- J Pharmacol Sci, 2023, 151(4):177-186
|
|
S5793 |
Motesanib (AMG-706)
|
Motesanib (AMG-706) is an orally bioavailable receptor tyrosine kinase inhibitor with IC50 values of 2 nM, 3 nM, 6 nM, 8 nM, 84 nM, 59 nM for VEGFR1, VEGFR2, VEGFR3, Kit, PDGFR and Ret, respectively. |
- Signal Transduct Target Ther, 2022, 7(1):147
- Front Cell Dev Biol, 2022, 10:836179
- J Pharm Sci, 2022, 111(8):2180-2190
|
|
S1181 |
ENMD-2076
|
ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to RET, SRC, NTRK1/TRKA, CSF1R/FMS, VEGFR2/KDR, FGFR and PDGFRα. ENMD-2076 inhibits the growth of a wide range of human solid tumor and hematopoietic cancer cell lines with IC50 from 0.025 to 0.7 μM, which induces apoptosis and G2/M phase arrest. Phase 2. |
- Cell, 2021, 184(2):334-351.e20
- Sci Adv, 2021, 7(4)eabd7851
- J Pediatr Hematol Oncol, 2019, 41(6):e359-e370
|
|
S1171 |
CYC116
|
CYC116 is a potent inhibitor of Aurora A/B with Ki of 8.0 nM/9.2 nM, is less potent to VEGFR2 (Ki of 44 nM), with 50-fold greater potency than CDKs, not active against PKA, Akt/PKB, PKC, no effect on GSK-3α/β, CK2, Plk1 and SAPK2A. Phase 1. |
- Sci Rep, 2024, 14(1):4303
- Cell Chem Biol, 2023, 30(8):987-998.e24
- Proc Natl Acad Sci U S A, 2022, 119(15):e2122512119
|
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S2859 |
Golvatinib (E7050)
|
Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2. |
- Int J Mol Sci, 2023, 24(11)9606
- Int J Mol Sci, 2022, 23(23)14884
- Cancer Sci, 2020, 111(10):3813-3823
|
|
S4686 |
Vitamin E
|
Vitamin E (D-alpha-Tocopherol) is a fat-soluble vitamin with potent antioxidant properties. It is a potent peroxyl radical scavenger and inhibits noncompetitively cyclooxygenase activity in many tissues, also inhibits angiogenesis and tumor dormancy through suppressing vascular endothelial growth factor (VEGF) gene transcription. |
- Signal Transduct Target Ther, 2024, 9(1):109
- Signal Transduct Target Ther, 2024, 9(1):109
- medRxiv, 2023, 10.1101/2023.12.01.23299102
|
|
S1220 |
OSI-930
|
OSI-930 is a potent inhibitor of Kit (c-Kit), KDR and CSF-1R with IC50 of 80 nM, 9 nM and 15 nM, respectively; also potent to Flt-1, c-Raf and Lck and low activity against PDGFRα/β, Flt-3 and Abl. Phase 1. |
- Nat Commun, 2024, 15(1):4739
- Cell Rep, 2019, 28(9):2331-2344
- Nat Biomed Eng, 2018, 2(8):578-588
|
|
S2622 |
PP121
|
PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. |
- Life Sci Alliance, 2021, 4(2)e202000882
- PLoS One, 2016, 11(10):e0164895
- PLoS One, 2016, 11(10):e0164895
|
|
S1557 |
KRN 633
|
KRN 633 is an ATP-competitive inhibitor of VEGFR1/2/3 with IC50 of 170 nM/160 nM/125 nM, weakly inhibits PDGFR-α/β and c-Kit, does not block the phosphorylation of FGFR-1, EGFR or c-Met in cell. |
- Aust Dent J, 2020, 10.1111/adj.12752
- J Med Invest, 2017, 64(3.4):262-265
- Oncotarget, 2016, 7(5):5985-99
|
|
S2231 |
Telatinib
|
Telatinib (BAY 57-9352) is a potent inhibitor of VEGFR2/3, c-Kit and PDGFRα with IC50 of 6 nM/4 nM, 1 nM and 15 nM, respectively. Phase 2. |
- Sci Adv, 2022, 8(6):eabg9455
- Leiden University Scholarly Publications, 2020, N/A
- Cell Stem Cell, 2019, 24(4):654-669
|
|
S5667 |
Fruquintinib
|
Fruquintinib is a small molecule inhibitor with strong potency and high selectivity against VEGFR family. It inhibits VEGFR 1, 2, 3, with IC50 values of 33 nM, 35 nM and 0.5 nM, respectively and shows only weak inhibition of RET, FGFR-1 and c-kit kinases. |
- EMBO J, 2024, 43(8):1519-1544
- Cancer Commun (Lond), 2023, 10.1002/cac2.12411
- Dev Cell, 2022, 57(12):1466-1481.e6
|
|
S8573 |
Sitravatinib (MGCD516)
|
Sitravatinib (MGCD516, MG-516) is a novel small molecule inhibitor targeting multiple RTKs involved in driving sarcoma cell growth, including c-Kit, PDGFRβ, PDGFRα, c-Met, and Axl. |
- JCI Insight, 2022, e148717
- Cancers (Basel), 2021, 13(21)5474
- Cancers (Basel), 2020, 12(1)
|
|
S7258 |
SKLB1002
|
SKLB1002 is a potent and ATP-competitive VEGFR2 inhibitor with IC50 of 32 nM. |
- Sci Adv, 2024, 10(20):eadl0633
- Sci Adv, 2024, 10(20):eadl0633
- Dis Model Mech, 2023, 16(5)dmm049571
|
|
S7003 |
AZD2932
|
AZD2932 is a potent and mutil-targeted protein tyrosine kinase inhibitor with IC50 of 8 nM, 4 nM, 7 nM, and 9 nM for VEGFR-2, PDGFRβ, Flt-3, and c-Kit, respectively.
|
- Cancer Res, 2020, canres.1992.2020
- Molecules, 2020, 8;25(9) pii: E2220
- Development, 2016, 143(23):4394-4404
|
|
S2366 |
Taxifolin (Dihydroquercetin)
|
Taxifolin, type I inhibitor for VEGFR-2 kinase, is a flavonoid in many plants such as Taxus chinensis, Siberian larch, Cedrus deodara and so on. |
- Sci Rep, 2020, 10(1):17311
- J Med Virol, 2019, 91(8):1440-1447
- Cytotechnology, 2016, 68(4):1633-40
|
|
S1138 |
Brivanib Alaninate (BMS-582664)
|
Brivanib alaninate (BMS-582664) is the prodrug of BMS-540215, an ATP-competitive inhibitor against VEGFR2 with IC50 of 25 nM. |
- Int J Oncol, 2014, 44(3):959-69
- Assay Drug Dev Technol, 2014, 12(9-10):514-26
|
|
S8189 |
BAW2881 (NVP-BAW2881)
|
BAW2881 (NVP-BAW2881) is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations. |
- JCI Insight, 2021, 143285
- J Cell Biochem, 2019, 120(4):5583-5596
|
|
S0504 |
SU14813
|
SU14813 (SU 014813) is a multiple receptor tyrosine kinase inhibitor with IC50 of 50 nM, 2 nM, 4 nM and 15 nM for VEGFR2, VEGFR1, PDGFRβ and Kit (c-Kit). SU14813 exhibits potent antiangiogenic and antitumor activity. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Adv Sci (Weinh), 2021, e2101848
|
|
S6535 |
SU1498
|
SU1498, a powerful inhibitor of KDR (IC50 = 0.7 μM), stimulates accumulation of phosphorylated ERK1/2 in endothelial cells. |
- Cell Metab, 2020, 5;31(5):892-908 e11
- Biol Open, 2018,
|
|
S8721 |
PDGFR inhibitor 1
|
PDGFR inhibitor 1 is an orally bioavailable switch pocket control inhibitor of wild-type and mutated forms of Kit (c-Kit) and PDGFR with potential antineoplastic activity. It also inhibits several other kinases, including VEGFR2, TIE2, PDGFR-beta and CSF1R, thereby further inhibiting tumor cell growth. |
- Elife, 2023, 12e79840
- Elife, 2023, 12e79840
- Oncogene, 2022, 41(20):2860-2872
|
|
S0278 |
SU5614
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SU5614 (Chloro-SU5416, Chloro-Semaxanib) is a small molecule receptor tyrosine kinases (RTK) inhibitor of VEGFR-2, c-kit, and both wild-type and mutant FLT3. SU5614 reduces cell proliferation and induces apoptosis. |
- Adv Sci (Weinh), 2021, e2101848
- Front Cell Dev Biol, 2021, 9:797047
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S6526 |
SKLB 610
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SKLB-610 is a multi-target inhibitor of the tyrosine kinases. It is most potent against VEGFR2 and exhibits slightly weaker inhibitor of FGFR2 and PDGFR. |
- Biomed Pharmacother, 2022, 149:112922
- Int J Mol Sci, 2022, 23(14)7853
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S6412 |
Altiratinib
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Altiratinib (DCC-2701) is a potent single-digit nanomolar inhibitor of TRK, Met (c-Met), TIE2, and VEGFR2 kinases with IC50 vaules of 0.9 nM, 4.6 nM, and 0.8 nM for TRKA, B, and C, respectively. It inhibits Met (c-Met) and Met (c-Met) mutant with IC50 values in the range of 0.3-6 nM. |
- Theranostics, 2021, 11(20):9918-9936
- Cold Spring Harb Mol Case Stud, 2021, 7(5)a006109
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S6514 |
SU5408
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SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and selective inhibitor of VEGFR2 Kinase with IC50 of 70 nM. |
- Transl Oncol, 2022, 25:101516
- J Dent Sci, 2022, 17(4):1471-1479
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S2201 |
BMS-794833
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BMS-794833 is a potent ATP competitive inhibitor of Met (c-Met)/VEGFR2 with IC50 of 1.7 nM/15 nM, also inhibits Ron, Axl and Flt3 with IC50 of <3 nM; a prodrug of BMS-817378. Phase 1. |
- Cancer Res, 2021, canres.1428.2021
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S0290 |
SU5204
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SU5204 is a tyrosine kinase inhibitor with IC50 of 4 μM and 51.5 μM for FLK-1 (VEGFR-2) and HER2, respectively. |
- Front Pharmacol, 2021, 12:804327
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S0487 |
Sulfatinib
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Sulfatinib is a potent and highly selective tyrosine kinase inhibitor against VEGFR1, VEGFR2, VEGFR3, FGFR1 and CSF1R with IC50 of 2 nM, 24 nM, 1 nM, 15 nM and 4 nM, respectively. Sulfatinib shows encouraging antitumor activity and manageable toxicities in patients with advanced NETs. |
- Front Oncol, 2023, 13:1158857
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S2018 |
ENMD-2076 L-(+)-Tartaric acid
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ENMD-2076 L-(+)-Tartaric acid is the tartaric acid of ENMD-2076, selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold more selective for Aurora A than Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα. Phase 2. |
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S6520 |
WHI-P180
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WHI-P180 is a multi-kinase inhibitor with IC50 values of 4.5 and 66 nM for the human proto-oncogene RET (c-RET) and kinase insert domain receptor (KDR), respectively. |
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S6543 |
ZD-4190
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ZD-4190 is a submicromolar inhibitor of VEGF RTK activity in vitro with IC50 values of 29 ± 4 nM and 708 ± 63 nM for KDR and Flt-1, respectively. |
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S7688 |
Ki20227
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Ki20227 is an orally active and highly selective inhibitor of c-Fms tyrosine kinase(CSF1R) with IC50 of 2 nM, 12 nM, 451 nM and 217 nM for c-Fms, vascular endothelial growth factor receptor-2 (KDR/VEGFR-2), stem cell factor receptor (c-Kit), and platelet-derived growth factor receptor beta (PDGFRβ), respectively. |
- Cancer Immunol Immunother, 2024, 73(5):76
- Cancer Immunol Immunother, 2024, 73(5):76
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S5272 |
Toceranib phosphate
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Toceranib phosphate (Palladia, SU11654), the phosphate salt of toceranib, is a selective inhibitor of the tyrosine kinase activity of several members of the split kinase RTK family, including Flk-1/KDR, PDGFR, and Kit with Ki values of 6 nM and 5 nM for Flk-1/KDR and PDGFRβ, respectively. |
- Front Vet Sci, 2024, 11:1392728
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S8188 |
BFH772
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BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM. |
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S0291 |
SU5208
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SU5208(3-[(Thien-2-yl)methylene]-2-indolinone) is an inhibitor of vascular endothelial growth factor receptor-2 (VEGFR2). |
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E2397 |
hVEGF-IN-1
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hVEGF-IN-1, a quinazoline derivative, specifically binds to the G-rich sequence in the internal ribosome entry site A (IRES-A) with a Kd of 0.928 μM, therefore destabilizes the G-quadruplex structure, , also hinders tumor cells migration and represses tumor growth by decreasing VEGF-A protein expression. |
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S8882 |
ODM-203
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ODM-203 is a selective inhibitor of FGFR and VEGFR with ic50s of 11 nM,16 nM,6 nM, 35 nM,26 nM,9 nM,5 nM for recombinant FGFR1, FGFR2, FGFR3,FGFR4, VEGFR1, VEGFR2 and VEGFR3, respectively. |
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S0763 |
Tyrphostin AG1433
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Tyrphostin AG1433 (AG1433, SU1433) is a selective platelet-derived growth factor receptor β (PDGFRβ) and vascular endothelial growth factor receptor 2 (VEGFR-2, Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. |
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S0765 |
MAZ51
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MAZ51 is a potent and selective inhibitor of vascular endothelial growth factor receptor (VEGFR)-3 (Flt-4) tyrosine kinase. MAZ51 induces cell rounding and G2/M cell cycle arrest in glioma cells through phosphorylation of Akt/GSK3β and activation of RhoA. MAZ51 inhibits the proliferation and induces the apoptosis of a variety of non-VEGFR-3-expressing tumor cell lines. |
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E0499 |
4SC-203
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4SC-203 (SC71710) is a multikinase inhibitor with potential antineoplastic activity. 4SC-203 selectively inhibits FMS-related tyrosine kinase 3 (FLT3/STK1), FLT3 mutated forms, and vascular endothelial growth factor receptors (VEGFRs).
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E2656 |
R1530
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R1530 is a highly potent, orally bioavailable, dual-acting mitosis/angiogenesis inhibitor for the treatment of solid tumors, which can inhibit vascular endothelial growth factor receptor 2 (VEGFR2) and fibroblast growth factor receptors 1 (FGFR1) with IC50s of 10 nM and 28 nM, respectively. |
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S9621 |
Donafenib (Sorafenib D3)
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Donafenib (Sorafenib D3, Bay 43-9006 D3, CM-4307) is the deuterium labeled Sorafenib. Sorafenib is a multikinase inhibitor IC50s of 6 nM, 15 nM, 20 nM and 22 nM for Raf-1, mVEGFR-2, mVEGFR-3 and B-RAF, respectively. |
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E1078 |
Emvododstat (PTC299)
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Emvododstat(PTC299), a post-transcriptional inhibitor of pathogenic VEGF and dihydroorotate dehydrogenase(DHODH), inhibits VEGFA mRNA translation and abnormal cell proliferation. In HeLa cells PTC299 inhibits hypoxia-induced VEGFA protein production with an EC50 of 1.64 nM. |
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S2211 |
AG-13958
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AG-13958 (AG-013958), a VEGFR tyrosine kinase inhibitor, is in clinical development with ST administration for treatment of choroidal neovascularization associated with age–related macular degeneration (AMD). |
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S5607 |
4,4'-Bis(4-aminophenoxy)biphenyl
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4,4'-Bis(4-aminophenoxy)biphenyl is a monomer for polyimide production. |
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S7647 |
Lucitanib (E3810) hydrochloride
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Lucitanib (E-3810, AL3810) hydrochloride is a dual inhibitor of Vascular endothelial growth factor receptor (VEGFR) and Fibroblast growth factor receptor (FGFR). Lucitanib hydrochloride (E-3810, AL3810) potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50 of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively. |
- Sci Rep, 2023, 13(1):20223
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E0616 |
Chiauranib
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Chiauranib (CS2164) selectively inhibits multiple kinase targets aurora B kinase (AURKB), colony-stimulating factor 1 receptor (CSF1R), and vascular endothelial growth factor receptor (VEGFR)/platelet-derived growth factor receptor (PDGFR)/c-Kit , thereby inhibiting the rapid proliferation of tumor cells, enhancing the antitumor immunity, and inhibiting tumor angiogenesis, to achieve the anti-tumor efficacy. |
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S6870 |
Ningetinib
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Ningetinib (CT-053, DE-120, CT053PTSA) is a potent, orally bioavailable inhibitor of tyrosine kinase with IC50 of 6.7 nM, 1.9 nM and <1.0 nM for c-Met, VEGFR2 and Axl, respectively. Ningetinib exhibits antitumor activity. |
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S6843 |
Vorolanib
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Vorolanib (X-82,CM082) is an oral, multikinase, dual inhibitor of vascular endothelial growth factor receptor (VEGFR) and platelet-derived growth factor receptor (PDGFR) with antiangiogenic and antineoplastic activities. |
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S6764 |
Pamufetinib (TAS-115)
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Pamufetinib (TAS-115) is a highly potent c-Met and VEGFR dual inhibitor with IC50s of 30 nM and 32 nM for recombinant VEGFR2 and recombinant MET, respectively. |
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S6939 |
Nastorazepide
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Nastorazepide (Z-360), a cholecystokinin-2/gastrin receptor (CCK2/gastrin receptor) antagonist, combines with gemcitabine prolonged survival and reduces gemcitabine-induced vascular endothelial growth factor (VEGF) expression in a pancreatic carcinoma orthotopic xenograft mouse. |
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S0377 |
CS-2660 (JNJ-38158471)
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CS-2660 (JNJ-38158471) is a well tolerated, orally available, highly selective VEGFR-2 inhibitor with IC50 of 40 nM. CS-2660 (JNJ-38158471) also inhibits closely related tyrosine kinases such as RET (c-RET) and Kit (c-Kit) with IC50 of 180 nM and 500 nM,while it has no significant activity (>1 microM) against VEGFR-1 and VEGFR-3. |
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E0534 |
WAY-340935
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WAY-340935 (VEGFR2-IN-2) can inhibit the function of VEGFR2 and the anti-proliferative activity against the H460 cell line is produced partly by interaction of VEGFR protein. |
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E3414 |
Semen litchi Extract
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Semen litchi Extract is extracted from Litchi chinensis, which has an anti-hepatoma effect and inhibits angiogenesis by targeting VEGFR in hepatocellular carcinoma. |
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E0207 |
Chebulinic acid
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Chebulinic acid, a phenolic compound isolated from Terminalia chebula fruit, is a novel Influenza viral neuraminidase inhibitor. Chebulinic acid is a antiangiogenic agent through inhibiting the actions of VEGF. Chebulinic acid shows antitumour activity.
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E3774 |
Chlorella Pyrenoidosa Extract
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Chlorella Pyrenoidosa Extract is extracted from Chlorella pyrenoidosa, which exerts a significant antiangiogenic activity was observed against VEGF-induced neovascularization and antiproliferative activity. |
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S6808 |
SU5205
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SU5205 is an inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 9.6 µM. |
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S6809 |
SU5214
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SU5214 is a inhibitor of VEGF receptor 2 (VEGFR2/FLK-1) with IC50 of 14.8 µM and EGFR with IC50 of 36.7 µm, respectively. |
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E1435New |
Tinengotinib
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Tinengotinib (TT-00420) is a novel multiple kinase inhibitor that strongly inhibits Aurora A/B with IC50 values of 1.2/3.3 nM respectively. It also exhibits potent inhibitory activity on FGFR1/2/3, VEGFR1, JAK1/2, and CSF1R and can be used to treat several prominent signaling pathways in triple-negative breast cancer(TNBC). |
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E0142 |
XL092
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XL092 (JUN04542) is an ATP-competitive inhibitor of multiple RTKs including MET, VEGFR2, AXL and MER, with IC50 values of 15 nM, 1.6 nM, 3.4 nM, and 7.2 nM in cell-based assays, respectively.
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