MLN2480


CAS No. : 1096708-71-2

MLN2480,1096708-71-2
Product Details
For research use only. Not Intended for Therapeutic Use!
Cat No:I000407
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:506.29
Target:Raf
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Appearance:Solid powder
Purity: > 98%
Cat No:I000407
Cas No:1096708-71-2
Product-Name:MLN2480
MDL No:MFCD22571730
InChI:InChI=1S/C17H12Cl2F3N7O2S/c1-6(28-15(31)12-11(19)13(23)27-5-26-12)16-25-4-9(32-16)14(30)29-10-2-7(17(20,21)22)8(18)3-24-10/h2-6H,1H3,(H,28,31)(H2,23,26,27)(H,24,29,30)/t6-/m1/s1
InChIKey:VWMJHAFYPMOMGF-ZCFIWIBFSA-N
SMILES:CC(C1=NC=C(S1)C(=O)NC2=NC=C(C(=C2)C(F)(F)F)Cl)NC(=O)C3=C(C(=NC=N3)N)Cl

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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