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SGX-523 1022150-57-7

Product Description

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Molecular Weight:

359.41 SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α. Phase 1.

Biological Activity

SGX-523 belongs to the class of c-Met/hepatocyte growth factor receptor
(HGFR) tyrosine kinase Inhibitors. SGX-523 stabilizes MET in a unique
inactive conformation that is inaccessible to Other protein kinases,
suggesting an explanation for its selectivity. SGX523 potently inhibits
the purified MET catalytic domain but not the closely related receptor
tyrosine kinase RON. SGX523 indicates ATP-competitive inhibition with
higher apparent affinity for the less active, unphosphorylated form of
MET [MET-KD(0P), with a Ki of 2.7 nM] versus the more active
phospho-enzyme [MET-KD(3P), with a Ki of 23 nM], a phenomenon consistent
with preferential binding to an inactive enzyme conformation.