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MLN2480 (BIIB-024) is an oral, selective pan-Raf kinase inhibitor. MLN2480 inhibits signaling pathway at high concentrations in the human malignant melanoma A-375 mutant B-raf Val600Glu cell line. In vivo, MLN2480 showed antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models. At 20-200mg MLN2480 PK data (13 pts) exhibited rapid absorption (median Tmax 2 hr), low fluctuation at steady state (mean peak to trough ratio 2.1), and mean accumulation half-life of 67 hr. MLN2480 is currently in a phase I trial.
| Molecular Weight | 506.29 |
| Formula | C17H12Cl2F3N7O2S |
| CAS Number | 1096708-71-2 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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