Chemical Name: 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)-(2S)-2-piperazineacetonitrile
Biological ActivityMRTX 849 is a mutant-selective inhibitor of KRASG12C (IC50 = 142 nM). MRTX 849 covalently binds to KRASG12C at the cysteine 12 residue and inhibits KRAS-dependent signal transduction by locking the protein in its inactive GDP-bound state. MRTX 849 induces pronounced tumor regression in 17 of 26 (65%) KRASG12C -positive cell lines and patient-derived xenograft models from multiple tumor types. It is orally bioavailable.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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