纯度:>98% by HPLC ,;NMR (Conforms)
分子式:C32H35ClFN7O2
分子量:604.13
溶剂:DMSO (>25 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):Covalent KRASG12C inhibitor
Function / Pharmacology: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