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
|
|
S2841 |
Bemcentinib (R428)
|
Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective). |
-
Nat Commun, 2024, 15(1):2818
-
Nat Commun, 2024, 15(1):6344
-
Theranostics, 2024, 14(7):2656-2674
|
|
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
|
|
S1561 |
BMS-777607
|
BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. |
-
Cancer Lett, 2024, 587:216692
-
Nat Commun, 2023, 14(1):4162
-
Oncogene, 2023, 42(21):1716-1727
|
|
S7754 |
Gilteritinib (ASP2215)
|
Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). |
-
Front Immunol, 2024, 15:1200461
-
Commun Biol, 2024, 7(1):412
-
iScience, 2024, 27(4):109576
|
|
S7846 |
Dubermatinib(TP-0903)
|
TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis. |
-
Cell Rep, 2023, 42(9):113067
-
Sci Adv, 2022, 8(20):eabk2746
-
Johns Hopkins University, 2022,
|
|
S7638 |
LDC1267
|
LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
|
-
Cell Metab, 2021, S1550-4131(21)00326-0
-
J Clin Invest, 2021, 131(8)e139434 139434
-
J Clin Invest, 2021, 131(8)139434
|
|
S7576 |
UNC2025 HCl
|
UNC2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
|
-
Immunity, 2023, 56(8):1778-1793.e10
-
Cell Rep, 2022, 38(13):110600
-
Cancers (Basel), 2021, 13(23)6072
|
|
S7014 |
Merestinib (LY2801653)
|
Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively. |
-
NPJ Breast Cancer, 2024, 10(1):65
-
Cancers (Basel), 2024, 16(12)2253
-
J Clin Invest, 2021, 131(11)146987
|
|
S9662 |
UNC2025
|
UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. |
-
Commun Biol, 2023, 6(1):916
-
Commun Biol, 2023, 6(1):916
-
Int J Mol Sci, 2023, 10.3390/ijms242115903
|
|
S8570 |
CEP-40783 (RXDX-106)
|
CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively. |
-
bioRxiv, 2023, 2023.10.20.563266
-
Mol Cancer Res, 2022, 20(4):542-555
-
J Oncol, 2022, 2022:2946929
|
|
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)
|
|
S7847 |
SGI-7079
|
SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance. |
-
Blood Cancer J, 2021, 11(5):93
-
Clin Cancer Res, 2017, 23(11):2713-2722
-
Oncotarget, 2017, 8(52):89761-89774
|
|
S7669 |
NPS-1034
|
NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. |
-
Nat Commun, 2023, 14(1):4162
-
J Med Chem, 2021, 64(6):3165-3184
-
Sci Rep, 2021, 11(1):19667
|
|
S7325 |
UNC2881
|
UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively. |
-
Cell Rep, 2020, 30(11):3671-3681
-
Front Immunol, 2019, 10:2647
|
|
S8404 |
S49076
|
S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. |
-
Mol Brain, 2020, 4;13(1):66
|
|
S8933 |
Tamnorzatinib (ONO-7475)
|
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active novel inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 of 0.7 nM and 1.0 nM for AXL and MER, respectively. ONO-7475 suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells. |
-
Cancer Lett, 2024, 587:216692
-
Cancer Sci, 2024, 10.1111/cas.16292
-
JTO Clin Res Rep, 2023, 4(6):100525
|
|
A2596 |
Tilvestamab (Anti-AXL / UFO)
|
Tilvestamab (Anti-AXL / UFO) is a humanized antibody targeting AXL.Tilvestamab can be used in cancer research, particularly in AXL overexpressing renal cell carcinomas. MW :146.16 KD. |
|
|
S0071 |
RU-301
|
RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively. |
|
|
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. |
|
|
E1818New |
PF-07265807
|
PF-07265807(TAM&Met-IN-1) is a dual inhibitor of AXL and MER, which exhibits anti-tumor effects. It also enhances the function of dendritic cells to cross-prime CD8+ T cells. |
|
|
A2586 |
Enapotamab (Anti-AXL / UFO)
|
Enapotamab(Anti-AXL / UFO) is a highly specific rabbit polyclonal antibody that targets receptor tyrosine kinase AXL (UFO). It demonstrates potent activity in immunotherapeutic strategy for the treatment of sarcomas. MW :145.42 KD. |
|
|
A2774 |
Mipasetamab (Anti-AXL / UFO)
|
Mipasetamab (Anti-AXL / UFO) is a human monoclonal IgG1κ antibody targeting AXL, a tyrosine kinase receptor, and an TAM receptor, which involves the synthesis of ADCT-601 (Mipasetamab uzoptirine), an AXL-targeted antibody-drug conjugate (ADC). MW: 145.78 kD. |
|
|
D4038 |
Enapotamab vedotin
|
Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker. |
|
|
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.
|
|
|
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
|
|
S2841 |
Bemcentinib (R428)
|
Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, >100-fold selective for Axl versus Abl. Selectivty for Axl is also greater than Mer and Tyro3 (50-to-100- fold more selective) and InsR, EGFR, HER2, and PDGFRβ (100- fold more selective). |
- Nat Commun, 2024, 15(1):2818
- Nat Commun, 2024, 15(1):6344
- Theranostics, 2024, 14(7):2656-2674
|
|
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
|
|
S1561 |
BMS-777607
|
BMS-777607 (BMS 817378) is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50 of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM in cell-free assays, 40-fold more selective for Met-related targets versus Lck, VEGFR-2, and TrkA/B, and more than 500-fold greater selectivity versus all other receptor and non receptor kinases. |
- Cancer Lett, 2024, 587:216692
- Nat Commun, 2023, 14(1):4162
- Oncogene, 2023, 42(21):1716-1727
|
|
S7754 |
Gilteritinib (ASP2215)
|
Gilteritinib (ASP2215) is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM). |
- Front Immunol, 2024, 15:1200461
- Commun Biol, 2024, 7(1):412
- iScience, 2024, 27(4):109576
|
|
S7846 |
Dubermatinib(TP-0903)
|
TP-0903 is a potent and selective AXL Inhibitor with IC50 of 27 nM. TP-0903 is highly effective in inducing apoptosis. |
- Cell Rep, 2023, 42(9):113067
- Sci Adv, 2022, 8(20):eabk2746
- Johns Hopkins University, 2022,
|
|
S7638 |
LDC1267
|
LDC1267 is a highly selective TAM kinase inhibitor with IC50 of <5 nM, 8 nM, and 29 nM for Mer, Tyro3, and Axl, respectively. Displays lower activity against Met, Aurora B, Lck, Src, and CDK8.
|
- Cell Metab, 2021, S1550-4131(21)00326-0
- J Clin Invest, 2021, 131(8)e139434 139434
- J Clin Invest, 2021, 131(8)139434
|
|
S7576 |
UNC2025 HCl
|
UNC2025 HCl is a potent and orally bioavailable dual MER/FLT3 inhibitor with IC50 of 0.74 nM and 0.8 nM, respectively, about 20-fold selectivity over Axl and Tyro3.
|
- Immunity, 2023, 56(8):1778-1793.e10
- Cell Rep, 2022, 38(13):110600
- Cancers (Basel), 2021, 13(23)6072
|
|
S7014 |
Merestinib (LY2801653)
|
Merestinib (LY2801653) is a type-II ATP competitive, slow-off inhibitor of Met (c-Met) tyrosine kinase with a dissociation constant (Ki) of 2 nM, a pharmacodynamic residence time (Koff) of 0.00132 min(-1) and t1/2 of 525 min. Merestinib (LY2801653) also inhibits MST1R, AXL, ROS1, MKNK1/2, FLT3, MERTK, DDR1 and DDR2 with IC50 of 11 nM, 2 nM, 23 nM, 7 nM, 7 nM, 10 nM, 0.1 nM and 7 nM, respectively. |
- NPJ Breast Cancer, 2024, 10(1):65
- Cancers (Basel), 2024, 16(12)2253
- J Clin Invest, 2021, 131(11)146987
|
|
S9662 |
UNC2025
|
UNC2025 is a potent and orally active dual inhibitor of FLT3 and MER with IC50 of 0.35 nM and 0.46 nM, respectively. UNC2025 also inhibits AXL, TRKA, TRKC, QIK, TYRO3, SLK, NuaK1, Kit (c-Kit) and Met (c-Met) with IC50 of 1.65 nM, 1.67 nM, 4.38 nM, 5.75 nM, 5.83 nM, 6.14 nM, 7.97 nM, 8.18 nM and 364 nM, respectively. |
- Commun Biol, 2023, 6(1):916
- Commun Biol, 2023, 6(1):916
- Int J Mol Sci, 2023, 10.3390/ijms242115903
|
|
S8570 |
CEP-40783 (RXDX-106)
|
CEP-40783 (RXDX-106) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/Met (c-Met) inhibitor displaying low nanomolar biochemical activity and slow (T1/2 >120 min) inhibitor off-rate in peptide phosphorylation assays and in vitro kinase binding assays, respectively. |
- bioRxiv, 2023, 2023.10.20.563266
- Mol Cancer Res, 2022, 20(4):542-555
- J Oncol, 2022, 2022:2946929
|
|
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)
|
|
S7847 |
SGI-7079
|
SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance. |
- Blood Cancer J, 2021, 11(5):93
- Clin Cancer Res, 2017, 23(11):2713-2722
- Oncotarget, 2017, 8(52):89761-89774
|
|
S7669 |
NPS-1034
|
NPS-1034 is a dual Met (c-Met)/Axl inhibitor with IC50 of 48 nM and 10.3 nM, respectively. |
- Nat Commun, 2023, 14(1):4162
- J Med Chem, 2021, 64(6):3165-3184
- Sci Rep, 2021, 11(1):19667
|
|
S7325 |
UNC2881
|
UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively. |
- Cell Rep, 2020, 30(11):3671-3681
- Front Immunol, 2019, 10:2647
|
|
S8404 |
S49076
|
S49076 is a novel, potent inhibitor of Met (c-Met), AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. |
- Mol Brain, 2020, 4;13(1):66
|
|
S8933 |
Tamnorzatinib (ONO-7475)
|
Tamnorzatinib (ONO-7475) is a potent, selective, and orally active novel inhibitor of Anexelekto(Axl)/MER tyrosine kinase with IC50 of 0.7 nM and 1.0 nM for AXL and MER, respectively. ONO-7475 suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. ONO-7475 arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells. |
- Cancer Lett, 2024, 587:216692
- Cancer Sci, 2024, 10.1111/cas.16292
- JTO Clin Res Rep, 2023, 4(6):100525
|
|
S0071 |
RU-301
|
RU-301 is a pan-TAM receptor (Axl, Tyro3 and Mertk) inhibitor that blocks the Axl receptor dimerization site with Kd of 12 μM and IC50 of 10 μM, respectively. |
|
|
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. |
|
|
E1818New |
PF-07265807
|
PF-07265807(TAM&Met-IN-1) is a dual inhibitor of AXL and MER, which exhibits anti-tumor effects. It also enhances the function of dendritic cells to cross-prime CD8+ T cells. |
|
|
D4038 |
Enapotamab vedotin
|
Enapotamab vedotin (EnaV, HuMAX-AXL-ADC) is an AXL-specific human IgG1 antibody conjugated to the microtubule disrupting agent monomethyl auristatin E (MMAE) through a protease cleavable valine-citrulline (vc) linker. |
|
|
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.
|
|
|