Discovery of Daraxonrasib (RMC-6236), a Potent and Orally Bioavailable RAS(ON) Multi-selective, Noncovalent Tri-complex Inhibitor for the Treatment of Patients with Multiple RAS-Addicted Cancers

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DOI:10.1021/acs.jmedchem.4c02314
作者：James Cregg, Anne V. Edwards, Stephanie Chang, Bianca J. Lee, John E. Knox, Aidan C. A. Tomlinson, Abby Marquez, Yang Liu, Rebecca Freilich, Naing Aay, Yingyun Wang, Lingyan Jiang, Jingjing Jiang, Zhi
文献类型：期刊论文
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American Chemical Society (ACS)

Abstract：Oncogenic RAS mutations are among the most common in human cancers. To target the active, GTP-bound state of RAS(ON) directly, we employed an innovative tri-complex inhibitor (TCI) modality.

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