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Mertk Inhibitors

Cat.No. Product Name Information Product Use Citations Product Validations
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
Verified customer review of UNC2250
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
S6839 MRX-2843 MRX-2843 (UNC2371) is an orally active dual inhibitor of tyrosine kinases MERTK and FLT3 with IC50 of 1.3 nM and 0.64 nM, respectively.
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.
E1744 UNC5293 UNC5293 is a potent, highly selective, orally available inhibitor of MER receptor tyrosine kinase (MERTK) with IC50 of 0.9 nM and Ki 0.19 nM.
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
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
Verified customer review of LDC1267
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
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
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
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
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.
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.