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
|
|
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
|
UNC-2025 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. |
-
Cancers (Basel), 2024, 16(12)2253
-
J Clin Invest, 2021, 131(11)146987
-
Mol Cancer Ther, 2021, molcanther.0344.2021
|
|
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
|
|
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
-
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. |
|
|
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. UNC2541 inhibits phosphorylated MerTK (pMerTK) with EC50 of 510 nM. |
|
|
E1744New |
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. |
|
|
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. |
|
|
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
|
|
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
|
UNC-2025 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. |
- Cancers (Basel), 2024, 16(12)2253
- J Clin Invest, 2021, 131(11)146987
- Mol Cancer Ther, 2021, molcanther.0344.2021
|
|
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
|
|
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
- 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. |
|
|
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. UNC2541 inhibits phosphorylated MerTK (pMerTK) with EC50 of 510 nM. |
|
|
E1744New |
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. |
|
|
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. |
|
|