KRAS-C9, K-Ras(G12C) Inhibitor

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.

Product information

CAS Number: 1469337-91-4

Molecular Weight: 513.78

Formula: C16H21ClIN3O4S

Chemical Name: N-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide

Smiles: COC1=CC(Cl)=C(I)C=C1NCC(=O)N1CCC(CC1)NS(=O)(=O)C=C

InChiKey: 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

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

KRAS-C9 was used at 10 µM final concentration in various in vitro assays.

References:

1. Ostrem JM, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. (2013) Nature. 503(7477):548-51.

Products are for research use only. Not for human use.

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