S1021 |
Dasatinib
|
Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity. |
-
Nature, 2024, 627(8003):407-415
-
Nature, 2024, 10.1038/s41586-024-07079-8
-
Mol Cancer, 2024, 23(1):240
|
|
S2475 |
Imatinib
|
Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy. |
-
Nat Biomed Eng, 2024, 10.1038/s41551-024-01204-8
-
Cell Rep Med, 2024, S2666-3791(24)00201-5
-
Elife, 2024, 12RP92324
|
|
S7782 |
Dasatinib Monohydrate
|
Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
|
-
bioRxiv, 2023, 2023.05.11.540170
-
bioRxiv, 2023, 2023.05.11.540170
-
Nat Cell Biol, 2022, 24(7):1049-1063
|
|
S1026 |
Imatinib Mesylate
|
Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. |
-
Mol Cancer, 2024, 23(1):240
-
Cell Rep, 2024, 43(3):113811
-
JCI Insight, 2024, 9(10):e162449.
|
|
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
|
|
S5254 |
Dasatinib hydrochloride
|
Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
-
Clin Transl Med, 2024, 14(5):e1660
-
Cell Death Dis, 2024, 15(8):603
-
Commun Biol, 2023, 6(1):872
|
|
S1033 |
Nilotinib
|
Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. |
-
Nat Commun, 2024, 15(1):651
-
Nat Commun, 2024, 15(1):2089
-
Elife, 2024, 12RP92324
|
|
S1014 |
Bosutinib
|
Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. |
-
Elife, 2024, 12RP92324
-
Front Immunol, 2024, 15:1425670
-
PLoS Pathog, 2024, 20(7):e1012170
|
|
S1048 |
Tozasertib (VX-680)
|
Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2. |
-
Cell Death Dis, 2024, 15(1):56
-
Cell Rep, 2024, 43(9):114739
-
Elife, 2024, 12RP92324
|
|
S2775 |
Nocodazole
|
Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis. |
-
Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
-
Nat Commun, 2024, 15(1):9771
-
Nucleic Acids Res, 2024, gkae605
|
|
S1107 |
Danusertib (PHA-739358)
|
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2. |
-
Elife, 2024, 12RP92324
-
Sci Rep, 2024, 14(1):4303
-
Environ Mol Mutagen, 2024, 10.1002/em.22604
|
|
S2243 |
Degrasyn (WP1130)
|
Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy. |
-
Clin Cancer Res, 2023, 29(2):446-457
-
Clin Cancer Res, 2023, 29(2):446-457
-
Cancer Cell Int, 2023, 23(1):207
|
|
S5205 |
Nilotinib hydrochloride
|
Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. |
-
Nat Commun, 2024, 15(1):2089
-
J Pharm Sci, 2022, 111(8):2180-2190
-
EMBO Mol Med, 2021, e11814
|
|
S1369 |
Bafetinib
|
Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. |
-
Elife, 2024, 12RP92324
-
Br J Haematol, 2023, 10.1111/bjh.18996
-
Int J Mol Sci, 2023, 10.3390/ijms241813863
|
|
S1134 |
AT9283
|
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
-
J Transl Med, 2024, 22(1):209
-
Int J Mol Sci, 2024, 25(5)2956
-
Sci Rep, 2024, 14(1):8200
|
|
S7526 |
GNF-5
|
GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM. |
-
Elife, 2024, 12RP92324
-
Nat Commun, 2023, 14(1):1885
-
Nat Commun, 2023, 14(1):1885
|
|
S7343 |
URMC-099
|
URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy. |
-
Cell Commun Signal, 2023, 21(1):82
-
Oncogene, 2023, 42(14):1132-1143.
-
Oncogenesis, 2023, 12(1):35
|
|
S2158 |
KW-2449
|
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1. |
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Cell Rep Med, 2022, 3(1):100492
-
Cancer Res, 2022, 82(11):2141-2155
|
|
S2634 |
Rebastinib (DCC-2036)
|
Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1. |
-
Elife, 2024, 12RP92324
-
Invest Ophthalmol Vis Sci, 2023, 64(10):6
-
Invest Ophthalmol Vis Sci, 2023, 64(10):6
|
|
S2202 |
NVP-BHG712
|
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. |
-
Nat Commun, 2024, 15(1):5894
-
Eur J Pharmacol, 2024, 983:177000
-
Cell Rep, 2022, 41(11):111827
|
|
S4895 |
Nilotinib hydrochloride monohydrate
|
Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. |
-
Nat Commun, 2024, 15(1):2089
-
J Pharm Sci, 2022, 111(8):2180-2190
-
EMBO Mol Med, 2021, e11814
|
|
S8555 |
Asciminib (ABL001)
|
Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1. |
-
Cell Death Differ, 2024, 10.1038/s41418-024-01339-w
-
Elife, 2024, 12RP92324
-
Cancers (Basel), 2024, 16(7)1288
|
|
S2899 |
GNF-2
|
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. |
-
Life Sci Alliance, 2023, 6(5)e202201605
-
Clin Sci (Lond), 2021, 135(19):2243-2263
-
Cell Chem Biol, 2018, 25(2):206-214
|
|
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
|
|
S7194 |
Olverembatinib (GZD824) dimesylate
|
Olverembatinib (GZD824) dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. |
-
Lab Invest, 2021, 10.1038/s41374-021-00683-6
-
Mol Pharmacol, 2020, 98(6):669-676
-
J Leukoc Biol, 2019, 106(2):455-466
|
|
S9141 |
Berbamine
|
Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA) induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). |
-
Pathogens, 2023, 12(6)845
-
Pathogens, 2023, 12(6)845
-
Prostate, 2023, 10.1002/pros.24632
|
|
S7269 |
PD173955
|
PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM. |
-
Sci Rep, 2022, 12(1):7
-
J Mol Biol, 2021, 434(2):167349
-
Science, 2020, 370(6513)eabc2754
|
|
S6662 |
AST-487 (NVP-AST487)
|
AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
-
Cancer Cell, 2022, S1535-6108(22)00312-9
-
Int J Mol Sci, 2022, 23(18)10819
-
Nat Commun, 2020, 21;11(1):1924
|
|
S8140 |
GNF-7
|
GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
|
-
PLoS Genet, 2024, 20(1):e1010851
-
Sci Rep, 2023, 13(1):5244
-
Sci Rep, 2023, 13(1):5244
|
|
S8134 |
Radotinib
|
Radotinib (IY-5511) is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
|
-
Drugs R D, 2019, 19(2):149-166
|
|
E1312 |
DPH
|
DPH is a potent cell permeable c-Abl activator, with an EC50 of 794 nM. |
|
|
S0373 |
CZC-8004
|
CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase. |
|
|
S8888 |
GMB-475
|
GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein. |
|
|
E0047 |
Vodobatinib (K0706)
|
Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.
|
|
|
E2202 |
1-Naphthyl PP1 hydrochloride
|
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively. |
|
|
S1272 |
XL228
|
XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively. |
|
|
S2642 |
1-Naphthyl PP1(1-NA-PP1)
|
1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
|
|
S6383 |
1-NM-PP1
|
1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. |
-
J Cell Biol, 2024, 223(11)e202403165
|
|
S9973 |
Flumatinib (HH-GV-678)
|
Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2 nM, 307.6 nM and 665.5 nM for c-Abl, PDGFRβand c-Kit, respectively.
|
|
|
S3609 |
Berbamine dihydrochloride
|
Berbamine (BA, BBM) dihydrochloride, a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA, BBM) dihydrochloride induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). |
-
Eur J Pharmacol, 2024, S0014-2999(24)00322-4
|
|
S1021 |
Dasatinib
|
Dasatinib is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. Dasatinib induces autophagy and apoptosis with anti-tumor activity. |
- Nature, 2024, 627(8003):407-415
- Nature, 2024, 10.1038/s41586-024-07079-8
- Mol Cancer, 2024, 23(1):240
|
|
S2475 |
Imatinib
|
Imatinib is a multi-target inhibitor of tyrosine kinase with inhibition for v-Abl, c-Kit and PDGFR, IC50 values are 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib (STI571) induces autophagy. |
- Nat Biomed Eng, 2024, 10.1038/s41551-024-01204-8
- Cell Rep Med, 2024, S2666-3791(24)00201-5
- Elife, 2024, 12RP92324
|
|
S7782 |
Dasatinib Monohydrate
|
Dasatinib Monohydrate (BMS-354825) is a novel, potent and multi-targeted inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM, respectively.
|
- bioRxiv, 2023, 2023.05.11.540170
- bioRxiv, 2023, 2023.05.11.540170
- Nat Cell Biol, 2022, 24(7):1049-1063
|
|
S1026 |
Imatinib Mesylate
|
Imatinib Mesylate is an orally bioavailability mesylate salt of Imatinib, which is a multi-target inhibitor of v-Abl, c-Kit and PDGFR with IC50 of 0.6 μM, 0.1 μM and 0.1 μM in cell-free or cell-based assays, respectively. Imatinib Mesylate (STI571) induces autophagy. |
- Mol Cancer, 2024, 23(1):240
- Cell Rep, 2024, 43(3):113811
- JCI Insight, 2024, 9(10):e162449.
|
|
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
|
|
S5254 |
Dasatinib hydrochloride
|
Dasatinib hydrochloride (BMS-354825) is the hydrochloride salt form of dasatinib, an inhibitor that targets Abl, Src and c-Kit, with IC50 of <1 nM, 0.8 nM and 79 nM in cell-free assays, respectively. |
- Clin Transl Med, 2024, 14(5):e1660
- Cell Death Dis, 2024, 15(8):603
- Commun Biol, 2023, 6(1):872
|
|
S1033 |
Nilotinib
|
Nilotinib is a selective Bcr-Abl inhibitor with IC50 less than 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. |
- Nat Commun, 2024, 15(1):651
- Nat Commun, 2024, 15(1):2089
- Elife, 2024, 12RP92324
|
|
S1014 |
Bosutinib
|
Bosutinib is a novel, dual Src/Abl inhibitor with IC50 of 1.2 nM and 1 nM in cell-free assays, respectively. Bosutinib also effectively decreases the activity of PI3K/AKT/mTOR, MAPK/ERK and JAK/STAT3 signaling pathways by blocking the phosphorylation levels of p-ERK, p-S6, and p-STAT3. Bosutinib promotes autophagy. |
- Elife, 2024, 12RP92324
- Front Immunol, 2024, 15:1425670
- PLoS Pathog, 2024, 20(7):e1012170
|
|
S1048 |
Tozasertib (VX-680)
|
Tozasertib (VX-680) is a pan-Aurora inhibitor, mostly against Aurora A with Kiapp of 0.6 nM in a cell-free assay, less potent towards Aurora B/Aurora C and 100-fold more selective for Aurora A than 55 other kinases. The only exceptions are Fms-related tyrosine kinase-3 (FLT-3) and BCR-ABL tyrosine kinase, which are inhibited by the Tozasertib with both Ki of 30 nM. Tozasertib induces apoptosis and autophagy. Phase 2. |
- Cell Death Dis, 2024, 15(1):56
- Cell Rep, 2024, 43(9):114739
- Elife, 2024, 12RP92324
|
|
S2775 |
Nocodazole
|
Nocodazole is a rapidly-reversible inhibitor of microtubule polymerization, also inhibits Abl, Abl(E255K) and Abl(T315I) with IC50 of 0.21 μM, 0.53 μM and 0.64 μM in cell-free assays, respectively. Nocodazole induces apoptosis. |
- Nat Cell Biol, 2024, 10.1038/s41556-024-01473-0
- Nat Commun, 2024, 15(1):9771
- Nucleic Acids Res, 2024, gkae605
|
|
S1107 |
Danusertib (PHA-739358)
|
Danusertib (PHA-739358) is an Aurora kinase inhibitor for Aurora A/B/C with IC50 of 13 nM/79 nM/61 nM in cell-free assays, modestly potent to Abl, TrkA, c-RET and FGFR1, and less potent to Lck, VEGFR2/3, c-Kit, CDK2, etc. Danusertib induces apoptosis, cell cycle arrest, and autophagy. Phase 2. |
- Elife, 2024, 12RP92324
- Sci Rep, 2024, 14(1):4303
- Environ Mol Mutagen, 2024, 10.1002/em.22604
|
|
S2243 |
Degrasyn (WP1130)
|
Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). Degrasyn (WP1130) induces apoptosis and blocks autophagy. |
- Clin Cancer Res, 2023, 29(2):446-457
- Clin Cancer Res, 2023, 29(2):446-457
- Cancer Cell Int, 2023, 23(1):207
|
|
S5205 |
Nilotinib hydrochloride
|
Nilotinib hydrochloride (AMN-107) is the hydrochloride salt form of nilotinib, an orally bioavailable Bcr-Abl tyrosine kinase inhibitor with antineoplastic activity. |
- Nat Commun, 2024, 15(1):2089
- J Pharm Sci, 2022, 111(8):2180-2190
- EMBO Mol Med, 2021, e11814
|
|
S1369 |
Bafetinib
|
Bafetinib is a potent and selective dual Bcr-Abl/Lyn inhibitor with IC50 of 5.8 nM/19 nM in cell-free assays, does not inhibit the phosphorylation of the T315I mutant and is less potent to PDGFR and c-Kit. |
- Elife, 2024, 12RP92324
- Br J Haematol, 2023, 10.1111/bjh.18996
- Int J Mol Sci, 2023, 10.3390/ijms241813863
|
|
S1134 |
AT9283
|
AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). |
- J Transl Med, 2024, 22(1):209
- Int J Mol Sci, 2024, 25(5)2956
- Sci Rep, 2024, 14(1):8200
|
|
S7526 |
GNF-5
|
GNF-5 is a selective and allosteric Bcr-Abl inhibitor with IC50 of 220 nM. |
- Elife, 2024, 12RP92324
- Nat Commun, 2023, 14(1):1885
- Nat Commun, 2023, 14(1):1885
|
|
S7343 |
URMC-099
|
URMC-099 is an orally bioavailable, brain penetrant mixed lineage kinase (MLK) inhibitor with IC50 of 19 nM, 42 nM, 14 nM, and 150 nM, for MLK1, MLK2, MLK3, and DLK, respectively, and also inhibits LRRK2 activity with IC50 of 11 nM. URMC-099 also inhibits ABL1 with IC50 of 6.8 nM. URMC-099 induces autophagy. |
- Cell Commun Signal, 2023, 21(1):82
- Oncogene, 2023, 42(14):1132-1143.
- Oncogenesis, 2023, 12(1):35
|
|
S2158 |
KW-2449
|
KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR. Phase 1. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Cell Rep Med, 2022, 3(1):100492
- Cancer Res, 2022, 82(11):2141-2155
|
|
S2634 |
Rebastinib (DCC-2036)
|
Rebastinib (DCC-2036) is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1. |
- Elife, 2024, 12RP92324
- Invest Ophthalmol Vis Sci, 2023, 64(10):6
- Invest Ophthalmol Vis Sci, 2023, 64(10):6
|
|
S2202 |
NVP-BHG712
|
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. |
- Nat Commun, 2024, 15(1):5894
- Eur J Pharmacol, 2024, 983:177000
- Cell Rep, 2022, 41(11):111827
|
|
S4895 |
Nilotinib hydrochloride monohydrate
|
Nilotinib (AMN-107, Tasigna) hydrochloride monohydrate is a selective and orally bioavailable inhibitor of Bcr-Abl with IC50 < 30 nM in Murine myeloid progenitor cells. Nilotinib induces autophagy through AMPK activition. |
- Nat Commun, 2024, 15(1):2089
- J Pharm Sci, 2022, 111(8):2180-2190
- EMBO Mol Med, 2021, e11814
|
|
S8555 |
Asciminib (ABL001)
|
Asciminib (ABL001) is a potent and selective allosteric ABL1 inhibitor with dissociation constant (Kd) of 0.5-0.8 nM and selectivity to the myristoyl pocket of ABL1. |
- Cell Death Differ, 2024, 10.1038/s41418-024-01339-w
- Elife, 2024, 12RP92324
- Cancers (Basel), 2024, 16(7)1288
|
|
S2899 |
GNF-2
|
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl, shows no activity to Flt3-ITD, Tel-PDGFR, TPR-MET and Tel-JAK1 transformed tumor cells. |
- Life Sci Alliance, 2023, 6(5)e202201605
- Clin Sci (Lond), 2021, 135(19):2243-2263
- Cell Chem Biol, 2018, 25(2):206-214
|
|
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
|
|
S7194 |
Olverembatinib (GZD824) dimesylate
|
Olverembatinib (GZD824) dimesylate is a novel orally bioavailable Bcr-Abl inhibitor for Bcr-Abl(WT) and Bcr-Abl(T315I) with IC50 of 0.34 nM and 0.68 nM, respectively. |
- Lab Invest, 2021, 10.1038/s41374-021-00683-6
- Mol Pharmacol, 2020, 98(6):669-676
- J Leukoc Biol, 2019, 106(2):455-466
|
|
S9141 |
Berbamine
|
Berbamine (BA), a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA) induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). |
- Pathogens, 2023, 12(6)845
- Pathogens, 2023, 12(6)845
- Prostate, 2023, 10.1002/pros.24632
|
|
S7269 |
PD173955
|
PD173955 is a potent Bcr-Abl inhibitor with IC50 of 1-2 nM, also inhibiting Src activity with IC50 of 22 nM. |
- Sci Rep, 2022, 12(1):7
- J Mol Biol, 2021, 434(2):167349
- Science, 2020, 370(6513)eabc2754
|
|
S6662 |
AST-487 (NVP-AST487)
|
AST-487 (NVP-AST487), a N,N'-diphenyl urea,is an ATP competitive inhibitor of Flt3 with ki of 0.12 μM.Besides FLT3, AST487 also inhibits RET,KDR,c-KIT,and c-ABL kinase with IC50 values below 1 μM. |
- Cancer Cell, 2022, S1535-6108(22)00312-9
- Int J Mol Sci, 2022, 23(18)10819
- Nat Commun, 2020, 21;11(1):1924
|
|
S8140 |
GNF-7
|
GNF-7 is a potent type-II kinase Bcr-Abl inhibitor with IC50 of <5 nM, 61 nM, 122 nM, 136 nM, and 133 nM for M351T, T315I, E255 V, G250E, and c-Abl, respectively.
|
- PLoS Genet, 2024, 20(1):e1010851
- Sci Rep, 2023, 13(1):5244
- Sci Rep, 2023, 13(1):5244
|
|
S8134 |
Radotinib
|
Radotinib (IY-5511) is a selective BCR-ABL1 tyrosine kinase inhibitor with IC50 of 34 nM, used to treat Chronic Myeloid Leukemia.
|
- Drugs R D, 2019, 19(2):149-166
|
|
S0373 |
CZC-8004
|
CZC-8004 (CZC-00008004) is a pan-kinase inhibitor that binds a range of tyrosine kinases including ABL kinase. |
|
|
E0047 |
Vodobatinib (K0706)
|
Vodobatinib (K0706, SCO-088, SUN K706, SUN-K0706) is a novel BCR-ABL1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants with IC50s of 167 nM, 154 nM,165 nM and 1967 nM for BCR-ABL1L248R, BCR-ABL1Y253H , BCR-ABL1E255V and BCR-ABL1T315I, respectively.
|
|
|
E2202 |
1-Naphthyl PP1 hydrochloride
|
1-Naphthyl PP1 hydrochloride (1-NA-PP 1 hydrochloride) is a selective inhibitor of Src family kinases, inhibits v-Src, c-Fyn, c-Abl, CDK2 and CAMKII with IC50s of 1.0, 0.6, 0.6, 18 and 22 μM, respectively. |
|
|
S1272 |
XL228
|
XL228 is a protein kinase inhibitor with IC50 of 5 nM, 1.4 nM, 3.1 nM, 1.6 nM, 6.1 nM and 2 nM for wild-type ABL kinase, ABL T315I, Aurora A, IGF-1R, SRC and LYN, respectively. |
|
|
S2642 |
1-Naphthyl PP1(1-NA-PP1)
|
1-Naphthyl PP1(1-NA-PP 1) is a highly selective and potent pan-PKD inhibitor with IC50 of 154.6 nM,133.4 nM and 109.4 nM for PKD1, PKD2 and PKD3, respectively. 1-Naphthyl PP1 is a selective inhibitor of Src family kinases (v-Src, c-Fyn) and the tyrosine kinase c-Abl with IC50 of 1.0 μM, 0.6 μM, 0.6 μM, 18 μM and 22 μM for v-Src, c-Fyn, c-Abl, CDK2 and CAMK II, respectively. |
|
|
S6383 |
1-NM-PP1
|
1-NM-PP1 (PP1 Analog II, 1NM-PP1, analogue 9) is a potent inhibitor of Src family kinases with IC50 of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively. 1-NM-PP1 also inhibits CDK2-as1, CAMKII-as1 and c-Abl-as2 with IC50 of 5.0 nM, 8.0 nM and 120 nM, respectively. |
- J Cell Biol, 2024, 223(11)e202403165
|
|
S9973 |
Flumatinib (HH-GV-678)
|
Flumatinib (HH-GV-678) is a novel inhibitor of Bcr-Abl with IC50 values of 1.2 nM, 307.6 nM and 665.5 nM for c-Abl, PDGFRβand c-Kit, respectively.
|
|
|
S3609 |
Berbamine dihydrochloride
|
Berbamine (BA, BBM) dihydrochloride, a traditional Chinese medicines extracted from Berberis amurensis (xiaoboan), is a novel inhibitor of bcr/abl fusion gene with potent anti-leukemia activity and also an inhibitor of NF-κB. Berbamine (BA, BBM) dihydrochloride induces apoptosis in human myeloma cells and inhibits the growth of cancer cells by targeting Ca²⁺/calmodulin-dependent protein kinase II (CaMKII). |
- Eur J Pharmacol, 2024, S0014-2999(24)00322-4
|
|