Ro 5126766

Description: Ro 5126766 (also known as CH5126766) is a novel, potent, first-in-class dual inhibitor of MEK/RAF mitogen-activated protein kinases (MAPKs) that allosterically inhibits BRAFV600E, CRAF, MEK, and BRAF with IC50 values of 8.2, 56, 160 nM, and 190 nM, respectively. As a protein kinase inhibitor specific for the Raf and MEK kinases, RO5126766 has potential anti-neoplastic activity. The inhibition of the kinase activities of Raf and MEK by RO5126766 resulted in the inhibition of of target gene transcription that promotes malignant transformation of cells. Both Raf and MEK are serine/threonine-specific kinases that respond to extracellular stimuli, such as mitogens, and are involved in the regulation of cellular processes, such as gene expression, mitosis, differentiation, and apoptosis.

References: Clin Cancer Res. 2012 Sep 1; 18(17):4806-19.; Oncotarget. 2018 Apr 13; 9(28):19597-19612.; Cancer Res. 2013 Jul 1; 73(13):4050-4060.