Name: SGX-523
CAS#: 1022150-57-7
Chemical Formula: C18H13N7S
Exact Mass: 359.09531
Molecular Weight: 359.41
Elemental Analysis: C, 60.15; H, 3.65; N, 27.28; S, 8.92
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.

Leave a Reply

Your email address will not be published. Required fields are marked *