Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein–Protein Interaction

John M. Ketcham; Jacob R. Haling; Shilpi Khare; Vickie Bowcut; David M. Briere; Aaron C. Burns; Robin J. Gunn; Anthony Ivetac; Jon Kuehler; Svitlana Kulyk; Jade Laguer; J. David Lawson; Krystal Moya; Natalie Nguyen; Lisa Rahbæk; Barbara Saechao; Christopher R. Smith; Niranjan Sudhakar; Nicole C. Thomas; Laura Vegar; Darin Vanderpool; Xiaolun Wang; Larry Yan; Peter Olson; James G. Christensen; Matthew A. Marx

doi:10.1021/acs.jmedchem.2c00741

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Abstract

PPI. Oral administration of MRTX0902 in combination with MRTX849 results in a significant increase in antitumor activity relative to that of either single agent, including tumor regressions in a subset of animals in the MIA PaCa-2 tumor mouse xenograft model.

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synapsesocial.com/papers/6a5bde889a157a8b1673c06d https://doi.org/10.1021/acs.jmedchem.2c00741

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Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein–Protein Interaction

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Design and Discovery of MRTX0902, a Potent, Selective, Brain-Penetrant, and Orally Bioavailable Inhibitor of the SOS1:KRAS Protein–Protein Interaction

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