| 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
|
|
| 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.
|
-
Journal of Hematology & Oncology, March 20, 2018, 43
-
Bioact Mater, 2024, 32:427-444
-
Redox Biol, 2022, 54:102366
|
|
| 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.
|
-
Frontiers in Bioengineering and Biotechnology, 2022, 788987
-
Cell Rep, 2020, 30(11):3671-3681
-
Cell Reports, 2020, 3671-3681
|
|
| 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.
|
-
Cancer Immunology Research, 2025, CIR-24-0335
-
Scientific Reports, 2024, 4125
-
Scientific Reports, 2024, 14:4125
|
|
| 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.
|
-
Nature Communications, 2024, 5292
|
|
| 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.
|
|
|
| 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.
|
-
Genes & Development, October 1, 2020, 1345-1358
-
Frontiers in Microbiology, June 29, 2020, 1292
-
Oncotarget, January 5, 2018, 6402-6415
|
|
| 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.
|
-
bioRxiv, 2025, 2025.07.18.665641
-
Immunity, 2023, 56(8):1778-1793.e10
-
International Journal of Molecular Sciences, 2023, 15903
|
|
| 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
-
Molecular Oncology, 2025, 2366-2387
-
NPJ Breast Cancer, 2024, 10(1):65
|
|
| 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.
|
-
Cell Reports, October 05, 2021, 109789
-
Journal of Clinical Investigation, November 01, 2018, 5034-5055
-
UNIVERSITY OF CALIFORNIA, 2023,
|
|