MRTX849, Covalent KRASG12C inhibitor

Product Details

Formal 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

Alternate Names: Adagrasib

Molecular Formula: C₃₂H₃₅ClFN₇O₂

Formula Weight: 604.1

CAS Number: 2326521-71-3

Purity: >98%

Formulation: Powder

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

Storage: -20°C

Stability: ≥ 2 years.

Applications

Covalent KRASG12C inhibitor

Functions

Potent (IC₅₀’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRAS^G12C inhibitor. It showed pronounced tumor regression in 17 of 26 KRAS^G12C-positive cell lines and xenograft models from multiple tumor types. MTRTX849 reversed the immunosuppressive tumor environment in a genetically modified mouse model and sensitized tumors to checkpoint inhibitor therapy in a genetically modified mouse KRAS^G12C lung adenocarcinoma model. It reversed ABCB1-mediated multidrug resistance in vitro and in vivo ^via attenuating ABCB1 efflux in drug-resistant cancer cells.

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)