MRTX849 is a potent, selective and covalent KRASG12C inhibitor with potential antineoplastic activity. It selectively modifies mutant cysteine 12 in GDP-bound KRASG12C, and inhibits KRAS-dependent signaling.

MRTX849 demonstrated pronounced tumor regression in 17 of 26 (65%) KRASG12C-positive cell line- and patient-derived xenograft models from multiple tumor types, and objective responses have been observed in patients with KRASG12C-positive lung and colon adenocarcinomas[1].

2326521-71-3

C32H35ClFN7O2

604.13

MRTX849;Adagrasib

[1]Jay B Fell , John P Fischer , Brian R Baer.Identification of the Clinical Development Candidate MRTX849, a Covalent KRAS G12C Inhibitor for the Treatment of Cancer.J Med Chem. 2020 Apr 6. [2]Jill Hallin , Lars D Engstrom , Lauren Hargis.The KRAS G12C Inhibitor MRTX849 Provides Insight Toward Therapeutic Susceptibility of KRAS-Mutant Cancers in Mouse Models and Patients.Cancer Discov. 2020 Jan;10(1):54-71.

[1]Yang F, Wen Y, Wang C, et al. Efficient targeted oncogenic KRASG12C degradation via first reversible-covalent PROTAC. European Journal of Medicinal Chemistry. 2022: 114088

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