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MLN 2480 CAS: 1096708-71-2

Category: Inhibitors
Product Name: MLN 2480
Cat No: I000407
CAS No: 1096708-71-2
Synonyms: 2-[(1R)-1-[(6-amino-5-chloropyrimidine-4-carbonyl)amino]ethyl]-N-[5-chloro-4-(trifluoromethyl)pyridin-2-yl]-1,3-thiazole-5-carboxamide
Molecular Formula: C17H12Cl2F3N7O2S
Molecular Weight: 506.3
SMILES: NC1=NC=NC(C(N[C@H](C)C2=NC=C(C(NC3=NC=C(Cl)C(C(F)(F)F)=C3)=O)S2)=O)=C1Cl
InChI: None
Solubility: 10 mM in DMSO
Target: Raf
Storage: powder
CAS 1096708-71-2,MLN 2480
  • Description

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.

  • Spec

Appearance:Solid powder
Purity: > 98%

  • References

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

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