bs-82733C

DATASHEET

Formulation White solid

Storage: -20°C

Product Information:

AMG 510 is a potent (IC50’s = 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.

Description:

CAS Number: 2296729-00-3 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 Molecular weight: 560.61 Formula: C30H30F2N6O3 Solubility: DMSO (>25 mg/ml) Physical Properties: White solid Purity: >98% by HPLC , NMR (Conforms)