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July 14, 2022Journal of Medicinal Chemistry96 citationsOpen Access

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

JKJohn M. KetchamJHJacob R. HalingSKShilpi Khare

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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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Ketcham et al. (2022) studied this question.

synapsesocial.com/papers/6a5bde889a157a8b1673c06dhttps://doi.org/10.1021/acs.jmedchem.2c00741
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