AMG 510, Covalent KRASG12C Inhibitor

Product Details

Formal 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

Molecular Formula: C₃₀H₃₀F₂N₆O₃

Formula Weight: 560.6

CAS Number: 2296729-00-3

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to 25 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

Covalent KRASG12C Inhibitor

Functions

AMG 510 is a potent (IC₅₀’s = 6 nM NCI-H358; 9 nM MIA PaCa-2) covalent KRAS^G12C inhibitor. 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. AMG 510 improved the efficacy of various other chemotherapeutic agents including inhibitors of HER kinases, EGFR, SHP2, PI3K, AKT, and MEK and synergized with immune checkpoint reagents. FDA approved for use in KRAS^G12C-positive non-small cell lung cancer. AMG 510 displayed efficacy alone and in combination with trametinib and/or buparlisib in pancreatic ductal adenocarcinoma cell lines.

Application Procedures

First dissolved in DMSO (25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 1 month.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)