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MRTX1133
CAS No. : 2621928-55-8
Biological Activity：MRTX1133 is a noncovalent, potent, and selective KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations[2].
Research Area：Cancer
Targets：Ras
Related Screening Libraries:Bioactive Compound Library Plus;GPCR/G Protein Compound Library;Kinase Inhibitor Library;Anti-Cancer Compound Library;Ferroptosis Compound Library;Glutamine Metabolism Compound Library;Anti-Lung Cancer Compound Library;Anti-Pancreatic Cancer Compound Library;Anti-Blood Cancer Compound Library;Angiogenesis-Related Compound Library;Anti-Liver Cancer Compound Library ;Anti-Colorectal Cancer Compound Library ;
Related Small Molecules:Deltarasin hydrochloride;ZINC09659342;KRAS G12C inhibitor 56;CCG-232601;KRAS G12D inhibitor 14;1A-116;KRAS G12D inhibitor 10;KRAS G12C inhibitor 20;KRAS G12C inhibitor 24;RM-018;KRAS G12C inhibitor 14;APS6-45;6H05;KRpep-2d TFA;KRAS G12C inhibitor 33;KRAS G12C inhibitor 53;K-Ras-IN-1;KRAS G12C inhibitor 41;KRAS G12C inhibitor 26;KRAS G12C inhibitor 16;KRAS inhibitor-11;SOS1-IN-13;BQU57;ZCL278;Digeranyl bisphosphonate;KRAS inhibitor-7;SOS1 activator 1;KRAS inhibitor-14;SAH-SOS1A
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