Mertk
Inhibitory Selectivity
Mertk Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7342 |
UNC2250UNC2250 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. |
UNC2250 induced suppression of MerTK-dependent signaling pathways in a dose-dependent manner. Z-138, Mino, and JVM-2 cells were treated with indicated concentrations of UNC2250 for 60 min; then, whole cell lysates were detected by western blot for phospholated and total MerTK, AKT, and p38.
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| S7638 |
LDC1267LDC1267 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. |
Time- and dose-dependent effects of LDC1267 in RSC96 cells.
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| S7325 |
UNC2881UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively. |
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| S8570 |
RXDX-106 (CEP-40783)RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/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. |
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| S8404 |
S49076S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. |
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| S8933New |
ONO-7475ONO-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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7342 |
UNC2250UNC2250 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. |
UNC2250 induced suppression of MerTK-dependent signaling pathways in a dose-dependent manner. Z-138, Mino, and JVM-2 cells were treated with indicated concentrations of UNC2250 for 60 min; then, whole cell lysates were detected by western blot for phospholated and total MerTK, AKT, and p38.
|
|
| S7638 |
LDC1267LDC1267 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. |
Time- and dose-dependent effects of LDC1267 in RSC96 cells.
|
|
| S7325 |
UNC2881UNC2881 is a specific Mer tyrosine kinase inhibitor with IC50 of 4.3 nM, about 83- and 58-fold selectivity over Axl and Tyro3, respectively. |
||
| S8570 |
RXDX-106 (CEP-40783)RXDX-106 (CEP-40783) is an orally-available, potent and selective TAM(TYRO3, AXL, MER)/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. |
||
| S8404 |
S49076S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nmol/L. |
||
| S8933New |
ONO-7475ONO-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. |
