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MRTX1257 (MRTX-1257)
MRTX1257 (MRTX-1257) is an orally available, potent, selective, and irreversible covalent inhibitor of KRAS G12C. It inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 0.9 nM, and is highly selective for the Cys12 of KRAS G12C in NCI-H358 cells over other cysteines; Demonstrates robust target engagement in vivo; Exhibits rapid and sustained efficacy against MIA PaCa-2 Xenocrafts, in which, at 100 mg/kg daily dose, leads to complete responses that are maintained >70 days after cessation of treatment. (ref 1).
Catalog NO: CT-MRTX1257
Synonym: MRTX1257
CAS NO: 2206736-04-9
Mol. Formula: C33H39N7O2
MW: 565.7 (or refer to Certificate of Analysis, batch-specific)
** in vivo Quality Material, 99.9-100% by achiral and chiral HPLCs. Hemihydrate, validated by a spot-on Quantitative Elemental Analysis, validated Cellular Potency (IC50 = 1 nM)* . Bulk!! Prompt.