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Background Information:
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).
APIM050053: MRTX1257 (MRTX-1257)
CAS No.: 2206736-04-9.
Molecular Formula: C33H39N7O2.
Molecular Weight: 565.7 (or refer to Certificate of Analysis, batch-specific).
Purity: >99.5% by Achiral and Chiral HPLCs.
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certificate of Analysis.
Storage: Refer to Certificate of Analysis.
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