Chemical Name: (1R)-6-Fluoro-7-(2-fluoro-6-hydroxyphenyl)-1-(4-methyl-2-propan-2-ylpyridin-3-yl)-4-[(2S)-2-methyl-4-prop-2-enoylpiperazin-1-yl]pyrido[2,3-d]pyrimidin-2-one. Alternate Names: Sotorasib
Covalent KRASG12C Inhibitor
Molecular Weight:
560.61
Purity:
>98% by HPLC , NMR (Conforms)
Form:
White solid
CAS Number:
[2296729-00-3]
Formula:
C30H30F2N6O3
Application Notes:
AMG 510 is a potent (IC50s = 6 nM NCI-H358, 9 nM MIA PaCa-2) covalent KRASG12C inhibitor.1,2 It significantly inhibited tumor growth in NCI-H358 and MIA PaCa-2 cell lines as well as CT-26 tumors (mouse syngeneic model) and caused tumor regression at higher doses.1 AMG 510 improved the efficacy of various other chemotherapeutic agents including inhibitors of HER kinases, EGFR, SHP2, PI3K, AKT, and MEK 1,3 and synergized with immune checkpoint reagents1. FDA approved for use in KRASG12C-positive non-small cell lung cancer. AMG 510 displayed efficacy alone4,5 and in combination5 with trametinib and/or buparlisib in pancreatic ductal adenocarcinoma cell lines.
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