An inhibitor of K-RasG12D
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MRTX-1133 is an inhibitor of K-RasG12D, a mutant form of K-Ras that accumulates in cancer cells.1 It selectively reduces ERK phosphorylation in AsPC-1 cells expressing mutant K-RasG12D (IC50 = 10.8 nM) over MiaPaCa-2 and SW620 cells expressing mutant K-RasG12C or K-RasG12V (IC50s = 456 and 4,400 nM, respectively) and MCF-7 cells expressing wild-type K-Ras in which ERK phosphorylation was not reduced.
1.Swiatnicki, M., Engel, L., Shrestha, R., et al.Profiling oncogenic KRAS mutant drugs with a cell-based Lumit p-ERK immunoassaySLAS Discov.S2472-5552(22)(2022)
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