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mrtx1257

" in TargetMol Product Catalog

Inhibitors & Agonists
1

MRTX-1257

T161432206736-04-9

MRTX-1257 is a selective, irreversible, and covalent inhibitor of KRAS G12C with an IC50 of 900 pM for KRAS-dependent ERK phosphorylation in H358 cells. MRTX-1257 demonstrated 31% bioavailability in the mouse, with free fraction exposures well above cellular potency, and 77% target engagement in a PK PD experiment.

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