Home Protein Tyrosine Kinase Axl

Axl Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
S2841 Bemcentinib (R428) Bemcentinib (R428, BGB324) is an inhibitor of Axl with IC50 of 14 nM, demonstrating >100-fold selectivity for Axl over Abl. This compound is also more than 50- to 100-fold selective for Axl versus Mer and Tyro3, and exhibits 100-fold greater selectivity compared to InsR, EGFR, HER2, and PDGFRβ.
Cell Stem Cell, 2025, S1934-5909(25)00265-6
J Clin Invest, 2025, e180893
Front Immunol, 2025, 16:1601420
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S7846 Dubermatinib(TP-0903) Dubermatinib (TP-0903) is a potent and selective AXL Inhibitor with IC50 of 27 nM, and it is highly effective in inducing apoptosis.
Cancer Sci, 2025, 10.1111/cas.70151
Biol Direct, 2025, 20(1):77
Mol Oncol, 2024, 10.1002/1878-0261.13749
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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. This compound 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
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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
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.
UNIVERSITY OF CALIFORNIA, 2023,
bioRxiv, 2023, 2023.10.20.563266
Mol Cancer Res, 2022, 20(4):542-555
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. This compound suppresses the emergence and maintenance of tolerant cells to the initial EGFR-TKIs, osimertinib or dacomitinib, in AXL-overexpressing EGFR-mutated NSCLC cells. It also arrests growth and kills FMS-like tyrosine kinase 3-internal tandem duplication mutant acute myeloid leukemia cells.
J Cell Mol Med, 2025, 29(1):e70321
Cancer Lett, 2024, 587:216692
Cancer Sci, 2024, 10.1111/cas.16292
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.
Cancers (Basel), 2025, 17(3)490
Blood Cancer J, 2021, 11(5):93
Clin Cancer Res, 2017, 23(11):2713-2722
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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.
E1818 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.
S1119 Cabozantinib (XL184) A potent VEGFR2 inhibitor with IC50 of 0.035 nM, Cabozantinib (XL184) 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. It induces PUMA-dependent apoptosis in colon cancer cells via AKT/GSK-3β/NF-κB signaling pathway.
Nat Commun, 2025, 16(1):509
Cell Death Differ, 2025, 10.1038/s41418-025-01510-x
Cell Death Dis, 2025, 16(1):76
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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. This compound induces apoptosis.
Sci Rep, 2025, 15(1):35889
bioRxiv, 2025, 2025.08.15.670608
Nat Neurosci, 2024, 10.1038/s41593-024-01604-8
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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.
Cell Rep, 2025, 44(8):116096
Front Immunol, 2025, 16:1601420
Endocrinology, 2025, 166(11)bqaf146
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S7754 ASP2215 (Gilteritinib) 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).
J Adv Res, 2025, S2090-1232(25)00134-1
Cancer Lett, 2025, 611:217446
Mol Ther Nucleic Acids, 2025, 36(3):102611
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. This compound 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.
Mol Oncol, 2025, 19(8):2366-2387
NPJ Breast Cancer, 2024, 10(1):65
Cancers (Basel), 2024, 16(12)2253
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.
Commun Biol, 2025, 8(1):1185
Res Sq, 2025, rs.3.rs-6431257
JCI Insight, 2022, e148717
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. This compound 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.
iScience, 2024, 27(7):110226
Commun Biol, 2023, 6(1):916
Int J Mol Sci, 2023, 10.3390/ijms242115903
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
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. This compound exhibits antitumor activity.
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.