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KRAS-C9, K-Ras(G12C) Inhibitor

Overview
Catalog # bs-60219c-2-mg-solid
Product Name KRAS-C9, K-Ras(G12C) Inhibitor
Specifications
Storage Buffer Powder
Storage Condition Store in dry, dark place at -20C for 1 year.
Target
Product Information Molecular Weight: 513.78

Formula: C16 H21 Cl I N3 O4 S

CAS Number: 1469337-91-4

InChi Key: ZGUSBCDCZNBNQT-UHFFFAOYSA-N

InChi: InChI=1S/C16H21ClIN3O4S/c1-3-26(23,24)20-11-4-6-21(7-5-11)16(22)10-19-14-9-13(18)12(17)8-15(14)25-2/h3,8-9,11,19-20H,1,4-7,10H2,2H3

Smiles: COC1C=C(Cl)C(I)=CC=1NCC(=O)N1CCC(CC1)NS(=O)(=O)C=C

Purity: 98.0

Solubility: DMSO up to 100 mM

Appearance: Solid Power.

Shelf Life: 1.0 years
Description KRAS-C9 is a potent and selective allosteric inhibitor of oncogenic K-Ras(G12C). It irreversibly binds to a common oncogenic mutant K-Ras(G12C) and blocks K-Ras(G12C) interactions, therefore does not affect the wild-type protein. Binding of KRAS-C9 to K-Ras(G12C) disrupts both switch-I and switch-II, subverting the native nucleotide preference to favour GDP over GTP and impairing binding to Raf. It can decrease viability and increase apoptosis of K-Ras(G12C)-containing cancer cell lines. KRAS-C9 provides structure-based validation of a new allosteric regulatory site on Ras that is targetable in a mutant-specific manner.