The MRTX1133 of use is selective and reversible KRAS-G12D inhibitors, which can inhibit KRAS G12D mutant cells in activated and inactivated state, but not KRAS wild-type tumor cells, MRTX1133 the specificity of KRAS G12D is more than 1000 times that of wild-type KRAS.
1. Wang X, et al. Identification of MRTX1133, a Noncovalent, Potent, and Selective KRAS G12D Inhibitor [published online ahead of print, 2021 Dec 10]. J Med Chem. 2021;10.1021/acs.jmedchem.1c01688.2. KRAS G12D Inhibitor: MRTX1133. [(accessed on 22 April 2021)];2021 Available online.
2-Naphthalenol, 4-[4-(3,8-diazabicyclo[3.2.1]oct-3-yl)-8-fluoro-2-[[(2R,7aS)-2-fluorotetrahydro-1H-pyrrolizin-7a(5H)-yl]methoxy]pyrido[4,3-d]pyrimidin-7-yl]-5-ethynyl-6-fluoro- - Reference Information
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MRTX1133 is a selective and reversible KRAS-G12D inhibitor, which can inhibit KRAS G12D mutant cells in activated and inactivated state, but does not inhibit KRAS wild-type tumor cells. the specificity of MRTX1133 for KRAS G12D is more than 1000 times that of wild-type KRAS.