bs-82732C

DATASHEET

Formulation Off-white solid

Storage: -20°C

Product Information:

MRTX849 is a potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced tumor regression in 17 of 26 KRASG12C-positive cell lines and xenograft models from multiple tumor types.2 MTRTX849 reversed the immunosuppressive tumor environment in a genetically modified mouse model and sensitized tumors to checkpoint inhibitor therapy in a genetically modified mouse KRASG12C lung adenocarcinoma model.3 It reversed ABCB1-mediated multidrug resistance in vitro and in vivo via attenuating ABCB1 efflux in drug-resistant cancer cells.4

Description:

CAS Number: 2326521-71-3 Chemical Name: 2-[(2S)-4-[7-(8-Chloronaphthalen-1-yl)-2-[[(2S)-1-methylpyrrolidin-2-yl]methoxy]-6,8-dihydro-5H-pyrido[3,4-d]pyrimidin-4-yl]-1-(2-fluoroprop-2-enoyl)piperazin-2-yl]acetonitrile Molecular weight: 604.13 Formula: C32H35ClFN7O2 Solubility: DMSO (>25 mg/ml) Physical Properties: White solid Purity: >98% by HPLC , NMR (Conforms)