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Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor - Nature Medicine

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Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor - Nature Medicine

Recent progress in targeting KRASG12C has provided both insight and inspiration for targeting alternative KRAS mutants. In this study, we evaluated the mechanism of action and anti-tumor efficacy of MRTX1133, a potent, selective and non-covalent KRASG12D inhibitor. MRTX1133 demonstrated a high-affinity interaction with GDP-loaded KRASG12D with KD and IC50 values of ~0.2 pM and <2 nM, respectively, and ~700-fold selectivity for binding to KRASG12D as compared to KRASWT.

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Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor - Nature Medicine

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Anti-tumor efficacy of a potent and selective non-covalent KRASG12D inhibitor - Nature Medicine

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