| CAS NO. |
Products Name |
|
|
| 698387-09-6 |
Neratinib (HKI-272) |
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| Neratinib (HKI-272) is a highly selective HER2 and EGFR inhibitor with IC50 of 59 nM and 92 nM; weakly inhibits KDR and Src, no significant inhibition to Akt, CDK1/2/4, IKK-2, MK-2, PDK1, c-Raf and c-Met. Phase 3 |
|
| 1032900-25-6 |
LDK378 |
more... |
| LDK378 is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. Phase 3. |
|
|
|
| 956905-27-4 |
PF04217903 |
more... |
| PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant). Phase 1. |
|
| 928037-13-2 |
Golvatinib（E7050) |
more... |
| Golvatinib(E7050) is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis. |
|
| 1025720-94-8 |
BMS777607 |
more... |
| BMS-777607 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, 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. Phase 1/2. |
|
| 1029712-80-8 |
INCB28060 |
more... |
| INCB28060 is a novel, ATP-competitive inhibitor of c-MET with IC50 of 0.13 nM, inactive against RONβ, as well as EGFR and HER-3. Phase 1. |
|
| 849217-64-7 |
Foretinib (GSK1363089) |
more... |
| Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR. Phase 2. |
|
| 943540-75-8 |
JNJ33877605 |
more... |
| JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases. Phase 1. |
|
| 1022150-57-7 |
SGX-523 |
more... |
| SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1. |
|
| 477575-56-7 |
PHA-665752 |
more... |
| PHA-665752 is a potent, selective and ATP-competitive c-Met inhibitor with IC50 of 9 nM, >50-fold selectivity for c-Met than RTKs or STKs. |
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