CAS No. : 1096708-71-2

Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000407
Molecular Formula:C₁₇H₁₂Cl₂F₃N₇O₂S
Molecular Weight:506.29
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Appearance:Solid powder
Purity: > 98%
Cat No:I000407
Cas No:1096708-71-2
MDL No:MFCD22571730

MLN 2480(BIIB-024) is an oral, selective pan-Raf kinase inhibitor in chinical trials.
IC50 value:
Target: pan-Raf
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.

[1]. Macauley, D, et al. Drugs Fut 2012, 37(6): 451

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