Product Overview
MRTX-1257 | T16143 | TargetMol Chemicals
CAS: 2206736-04-9
Smiles: CN1CCC[C@H]1COc1nc2CN(CCc2c(n1)N1CCN([C@@H](CC#N)C1)C(=O)C=C)c1cccc2cccc(C)c12
Formula: C33H39N7O2
Pathway: GPCR/G Protein|||MAPK
Target: Ras
Receptor: N/A
Bioactivity: MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C. It has an IC50 of 900 pM for KRAS dependent ERK phosphorylation in H358 cells. MRTX1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above the cellular potency In a PK/PD experiment, 77% target engagement.
Molecular Weight: 565, 722
