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.
Molekulargewicht:
565.71
Reinheit:
96.59%
CAS Nummer:
[2206736-04-9]
Formel:
C33H39N7O2
Target-Kategorie:
Ras|||Kras
T16143
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