Article
Antitumor Properties of RAF709, a Highly Selective and Potent Inhibitor of RAF Kinase Dimers, in Tumors Driven by Mutant RAS or BRAF.
Cancer research - 15 Mar 2018
Shao Wenlin, Mishina Yuji M, Feng Yun, Caponigro Giordano, Cooke Vesselina G, Rivera Stacy, Wang Yingyun, Shen Fang, Korn Joshua M, Mathews Griner Lesley A, Nishiguchi Gisele, Rico Alice, Tellew John, Haling Jacob R, Aversa Robert, Polyakov Valery, Zang Richard, Hekmat-Nejad Mohammad, Amiri Payman, Singh Mallika, Keen Nicholas, Dillon Michael P, Lees Emma, Ramurthy Savithri, Sellers William R, Stuart Darrin D
Abstract excerpt
Resistance to the RAF inhibitor vemurafenib arises commonly in melanomas driven by the activated BRAF oncogene. Here, we report antitumor properties of RAF709, a novel ATP-competitive kinase inhibitor with high potency and selectivity against RAF kinases. RAF709 exhibited a mode of RAF inhibition distinct from RAF monomer inhibitors such as vemurafenib, showing equal activity against both RAF monomers and dimers....
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