Article
AZD4625 is a Potent and Selective Inhibitor of KRASG12C.
Molecular cancer therapeutics - 7 Oct 2022
Chakraborty Atanu, Hanson Lyndsey, Robinson David, Lewis Hilary, Bickerton Sue, Davies Michael, Polanski Radoslaw, Whiteley Rebecca, Koers Alex, Atkinson James, Baker Tamara, Del Barco Barrantes Ivan, Ciotta Giovanni, Kettle Jason G, Magiera Lukasz, Martins Carla P, Peter Alison, Wigmore Eleanor, Underwood Zoe, Cosulich Sabina, Niedbala Michael, Ross Sarah
Abstract excerpt
AZD4625 is a potent, selective, and orally bioavailable inhibitor of oncogenic KRASG12C as demonstrated in cellular assays and in vivo in preclinical cell line-derived and patient-derived xenograft models. In vitro and cellular assays have shown selective binding and inhibition of the KRASG12C mutant isoform, which carries a glycine to cysteine mutation at residue 12, with no binding and inhibition of wild-type...
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