Discovery of MK-1084: An Orally Bioavailable and Low-Dose KRASG12C Inhibitor

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DOI:10.1021/acs.jmedchem.4c00572
作者：Xiaoshen Ma*,?David L. Sloman*,?Ruchia Duggal*,?Kenneth D. Anderson,?Jeanine E. Ballard,?Indu Bharathan,?Christopher Brynczka,?Symon Gathiaka,?Timothy J. Henderson,?Thomas W. Lyons,?Richard Miller,?Er
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American Chemical Society (ACS)

Abstract：Oncogenic mutations in the RAS gene account for 30% of all human tumors; more than 60% of which present as KRAS mutations at the hotspot codon 12. After decades of intense pursuit, a covalen

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