MLN 2480(BIIB-024)|cas 1096708-71-2|DC Chemicals

MLN 2480(BIIB-024)|cas 1096708-71-2|DC Chemicals

MLN 2480(BIIB-024) is an oral, selective pan-Raf kinase inhibitor in chinical trials.

Product Name: MLN 2480(BIIB-024)|Cat No. DC9302|cas: 1096708-71-2|Other names: BIIB-024; MLN2480; MLN-2480| Molecule formular: C17H12Cl2F3N7O2SMolecule Weight: 506.29

in vitro: MLN-2480 is active against wild-type B-raf and B-raf Val600Glu in vitro. MLN-2480 is found to activate phosphorylated MEK at very low concentrations, but at higher concentrations MLN-2480 inhibits this same activity. MLN-2480 inhibits signaling pathway at high concentrations in the human malignant melanoma A-375 mutant B-raf Val600Glu cell line. The inhibitory effects of MLN-2480 are found to vary across models and genetic contexts; MLN-2480 only modestly inhibits PRAK. MLN-2480 in combination with TAK-733 demonstrates synergy in NRAS mutant human malignant melanoma cell lines (SK-MEL-2), with high levels of apoptotic biomarkers observed.
in vivo: MLN-2480 (37.5 mg/kg) is well tolerated in a tumor xenograft model. The combination of MLN-2480 (12.5 mg) and TAK-733 (1 mg/kg) is effective in an SK-MEL-30 xenograft model, but monotherapy with either compound produced negligible effects.