MRTX-849

MRTX-849

CAT N°: 31440
Price:

From 66.00 56.10

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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