Home Protein Tyrosine Kinase TAM receptors (Tyro-3,Axl,and Mertk)

TAM receptors (Tyro-3,Axl,and Mertk) Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
E7462New Merestinib dihydrochloride Merestinib dihydrochloride (LY2801653 dihydrochloride) is an orally bioavailable, potent c-Met inhibitor exhibiting a Ki value of 2 nM. This compound demonstrates antitumor activity and inhibits multiple kinases, including MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM), and MKNK1/2 (IC50=7 nM).
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
Verified customer review of Cabozantinib (XL184)
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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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
Verified customer review of Cabozantinib malate
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
S7067 Tepotinib Tepotinib is a potent and selective c-Met inhibitor with IC50 of 4 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. This compound induces autophagy. Phase 1.
J Biomed Sci, 2025, 32(1):94
Cell Oncol (Dordr), 2025, 10.1007/s13402-025-01097-y
Lung Cancer, 2025, 201:108415
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S8696 2-D08 2-D08 (2',3',4'-trihydroxy flavone) is a cell permeable, mechanistically unique inhibitor of protein sumoylation. This compound is a cell permeable, mechanistically unique inhibitor of protein sumoylation.
Commun Biol, 2025, 8(1):1118
Int Immunopharmacol, 2025, 149:114187
Nat Commun, 2024, 15(1):9195
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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S1497 Pralatrexate Pralatrexate is an antifolate, and structurally a folate analog. Its IC50 is < 300 nM in some cell lines. This compound induces tumor cell apoptosis.
Cell Rep Med, 2025, S2666-3791(25)00102-8
Br J Haematol, 2024, 10.1111/bjh.19658
Discov Oncol, 2024, 15(1):709
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S7342 UNC2250 UNC2250 is a potent and selective Mer inhibitor with IC50 of 1.7 nM, about 160- and 60-fold selectivity over the closely related kinases Axl/Tyro3.
Bioact Mater, 2024, 32:427-444
Redox Biol, 2022, 54:102366
Front Immunol, 2022, 13:942640
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S8619 NCT-503 NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with the IC50 value of 2.5 μM. It is inactive against a panel of other dehydrogenases and shows minimal cross-reactivity in a panel of 168 GPCRs.
Adv Mater, 2025, e2502617
Cell Rep, 2024, 43(8):114517
J Cancer, 2024, 15(9):2538-2548
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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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
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
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
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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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
S7545 G-749 G-749 is a novel and potent FLT3 inhibitor with IC50 of 0.4 nM, 0.6 nM and 1 nM for FLT3 (WT), FLT3 (D835Y), and Mer, respectively, showing lower potency against other tyrosine kinases.
Front Pharmacol, 2021, 12:730241
E5942New UNC9426 UNC9426 (compound 12) is a potent and orally bioavailable inhibitor of TYRO3 with an IC50 of 2.1 nM. It reduces platelet aggregation without prolonging bleeding time and effectively suppresses TYRO3-mediated signalling pathways in tumor cells and macrophages.
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. This compound exhibits antitumor activity.
S4487 Gilteritinib hemifumarate Gilteritinib (ASP2215) hemifumarate is a potent and ATP-competitive FLT3/AXL inhibitor with IC50 of 0.29 nM/0.73 nM, respectively.
E4914 Cabozantinib hydrochloride Cabozantinib hydrochloride(XL184, BMS-907351 hydrochloride) is a potent small-molecule kinase inhibitor of c-MET and VEGFR2 with an IC50 of 1.3 nM, 0.035 nM respectively. It also inhibits RET, KIT, AXL, Tie2 and FLT3 with an IC50's of 5.2 nM, 4.6 nM, 7 nM, 14.3 nM, 11.3nM respectively. It can be promising agent for inhibiting tumor angiogenesis and metastasis in cancers with dysregulated MET and VEGFR signaling.
S0439 UNC2541 UNC2541 is a potent and specific inhibitor of Mer tyrosine kinase (MerTK) that binds in the MerTK ATP pocket with IC50 of 4.4 nM. This compound inhibits phosphorylated MerTK (pMerTK) with EC50 of 510 nM.
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.