Catalog No.: PC-72958Not For Human Use, Lab Use Only.
ASP2453 (ASP-2453) is a novel potent, selective and covalent KRAS G12C inhibitor, inhibits SOS-mediated interaction between KRAS G12C and Raf with IC50 of 40 nM.
ASP2453 (ASP-2453) is a novel potent, selective and covalent KRAS G12C inhibitor, inhibits SOS-mediated interaction between KRAS G12C and Raf with IC50 of 40 nM.
ASP2453 potently and selectively inhibited KRAS G12C-mediated growth, KRAS activation and downstream signalling in vitro and in vivo, and improved the anti-tumour effects of targeted agents and immune checkpoint inhibitors.
ASP2453 had more rapid binding kinetics to KRAS G12C protein and showed more potent inhibitory effects on KRAS activation and cell proliferation after washout than AMG 510.
ASP2453 also induced tumour regression in an AMG 510-resistant xenograft model.
