SGX523
| CAS No. | 1072116-01-8 | Cat. No. | BCP21622 |
| Name | SGX523 | ||
| Synonyms | SGX-523; SGX 523; | ||
| Formula | C18H13N7S | M. Wt | 359.41 |
| Description | SGX523 is a novel, ATP-competitive kinase inhibitor remarkable for its exquisite selectivity for MET. SGX523 potently inhibited MET with an IC50 of 4 nmol/L and is >1,000-fold selective versus the >200-fold selectivity of other protein kinases tested in biochemical assays. Crystallographic study revealed that SGX523 stabilizes MET in a unique inactive conformation that is inaccessible to other protein kinases, suggesting an explanation for the selectivity. SGX523 inhibited MET-mediated signaling, cell proliferation, and cell migration at nanomolar concentrations but had no effect on signaling dependent on other protein kinases, including the closely related RON, even at micromolar concentrations. | ||
| Pathways | Angiogenesis/Protein Tyrosine Kinase | ||
| Targets | c Met | ||
Structure
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