LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors.

doi:10.1158/1078-0432.CCR-20-2563

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Article

LXH254, a Potent and Selective ARAF-Sparing Inhibitor of BRAF and CRAF for the Treatment of MAPK-Driven Tumors.

Clinical cancer research : an official journal of the American Association for Cancer Research - 1 Apr 2021

Monaco Kelli-Ann, Delach Scott, Yuan Jing, Mishina Yuji, Fordjour Paul, Labrot Emma, McKay Daniel, Guo Ribo, Higgins Stacy, Wang Hui Qin, Liang Jinsheng, Bui Karen, Green John, Aspesi Peter, Ambrose Jessi, Mapa Felipa, Griner Lesley, Jaskelioff Mariela, Fuller John, Crawford Kenneth, Pardee Gwynn, Widger Stephania, Hammerman Peter S, Engelman Jeffrey A, Stuart Darrin D, Cooke Vesselina G, Caponigro Giordano

Abstract excerpt

PURPOSE: Targeting RAF for antitumor therapy in RAS-mutant tumors holds promise. Herein, we describe in detail novel properties of the type II RAF inhibitor, LXH254. EXPERIMENTAL DESIGN: LXH254 was profiled in biochemical, in vitro, and in vivo assays, including examining the activities of the drug in a large panel of cancer-derived cell lines and a comprehensive set of in vivo models. In addition, activity of...

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PMID: 33355204
DOI: 10.1158/1078-0432.CCR-20-2563

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