A covalent inhibitor of K-RasG12C; binds to and stabilizes GDP-bound inactive K-RasG12C in an electrophoretic mobility shift assay from 2-15.6 nM; reduces phosphorylation of the K-Ras targets ERK and S6 in MIA PaCa-2 cancer cells from 33-1

MRTX-849 – 1 mg

Brand:
Cayman
CAS:
2326521-71-3
Storage:
-20
UN-No:
Non-Hazardous - /

MRTX-849 is a covalent inhibitor of K-RasG12C, a mutant form of K-Ras that accumulates in cancer cells.{52771} It binds to and stabilizes GDP-bound inactive K-RasG12C in an electrophoretic mobility shift assay when used at concentrations ranging from 2 to 15.6 nM. MRTX-849 (33-1,000 nM) reduces phosphorylation of the K-Ras targets ERK and S6 in MIA PaCa-2 cancer cells, which express K-RasG12C. In vivo, MRTX-849 (100 mg/kg) reduces tumor volume in 17 K-RasG12C-expressing lung, colon, pancreatic, cervical, and esophageal cancer mouse xenograft models but not wild-type K-Ras-expressing A549, HCT116, and H1299 mouse xenograft models.  

 

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SKU: 31440 - 1 mg Category:

Description

A covalent inhibitor of K-RasG12C; binds to and stabilizes GDP-bound inactive K-RasG12C in an electrophoretic mobility shift assay from 2-15.6 nM; reduces phosphorylation of the K-Ras targets ERK and S6 in MIA PaCa-2 cancer cells from 33-1,000 nM; reduces tumor volume in 17 K-RasG12C-expressing lung, colon, pancreatic, cervical, and esophageal cancer mouse xenograft models at 100 mg/kg

Formal name: (2S)-4-[7-(8-chloro-1-naphthalenyl)-5,6,7,8-tetrahydro-2-[[(2S)-1-methyl-2-pyrrolidinyl]methoxy]pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoro-1-oxo-2-propen-1-yl)-2-piperazineacetonitrile

Synonyms: 

Molecular weight: 604.1

CAS: 2326521-71-3

Purity: ≥98%

Formulation: A crystalline solid

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