Tovorafenib

Tovorafenib (TAK-580, MLN 2480) is an orally active and selective inhibitor of pan-Raf kinase. Tovorafenib can be used for the study of glioma^[1]. In Vitro:Tovorafenib (TAK-580, MLN 2480) has effect on reversing feedback activation of MEK in response to TAK-733, leading to more concerted MAPK pathway inhibition^[1]. In Vivo:Tovorafenib (TAK-580, MLN 2480) inhibits MAPK pathway signaling in BRAF mutant and some RAS mutant preclinical cancer models at concentrations that are tolerated in vivo. TAK-580 (MLN 2480) is most potent in BRAF mutant melanoma models but also has single agent activity in some RAS mutant models. The combination of MLN2480 with TAK-733 inhibits the growth of a broader range of RAS mutant tumor models than single agent TAK-580 (MLN 2480), including primary human tumor xenograft models of melanoma and CRC^[1].