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The SOS1 Inhibitor MRTX0902 Blocks KRAS Activation and Demonstrates Antitumor Activity in Cancers Dependent on KRAS Nucleotide Loading.
Sudhakar N, Yan L, Qiryaqos F, Engstrom LD, Laguer J, Calinisan A, Hebbert A, Waters L, Moya K, Bowcut V, Vegar L, Ketcham JM, Ivetac A, Smith CR, Lawson JD, Rahbaek L, Clarine J, Nguyen N, Saechao B, Parker C, Elliott AJ, Vanderpool D, He L, Hover LD, Fernandez-Banet J, Coma S, Pachter JA, Hallin J, Marx MA, Briere DM, Christensen JG, Olson P, Haling J, Khare S. Sudhakar N, et al. Among authors: yan l. Mol Cancer Ther. 2024 Apr 19. doi: 10.1158/1535-7163.MCT-23-0870. Online ahead of print. Mol Cancer Ther. 2024. PMID: 38641404
Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein-Protein Interaction.
Ketcham JM, Haling J, Khare S, Bowcut V, Briere DM, Burns AC, Gunn RJ, Ivetac A, Kuehler J, Kulyk S, Laguer J, Lawson JD, Moya K, Nguyen N, Rahbaek L, Saechao B, Smith CR, Sudhakar N, Thomas NC, Vegar L, Vanderpool D, Wang X, Yan L, Olson P, Christensen JG, Marx MA. Ketcham JM, et al. Among authors: yan l. J Med Chem. 2022 Jul 28;65(14):9678-9690. doi: 10.1021/acs.jmedchem.2c00741. Epub 2022 Jul 14. J Med Chem. 2022. PMID: 35833726 Free PMC article.