An oral pan-Raf kinase inhibitor
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MLN2480

Item No. 19675

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
6-amino-5-chloro-N-[(1R)-1-[5-[[[5-chloro-4-(trifluoromethyl)-2-pyridinyl]amino]carbonyl]-2-thiazolyl]ethyl]-4-pyrimidinecarboxamide
CAS Number
1096708-71-2
Synonyms
  • BIIB-024
  • TAK-580
  • Tovorafenib
Molecular Formula
C17H12Cl2F3N7O2S
Formula Weight
506.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:4): 0.2 mg/mlDMSO: 20 mg/mlEthanol: 20 mg/ml
λmax
237, 276, 303 nm
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 Code
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
InChi Key
VWMJHAFYPMOMGF-ZCFIWIBFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    Product Description

    MLN2480 is an orally bioavailable pan-Raf kinase inhibitor that inhibits MAP kinase pathway signaling in BRAF-mutant melanoma models.1 It shows antitumor activity in melanoma, colon, lung, and pancreatic cancer xenograft models.2 MLN2480 demonstrates synergistic activity with TAK-733, an allosteric MEK kinase inhibitor.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Whittaker, S.R., Cowley, G.S., Wagner, S., et al. Combined pan-RAF and MEK inhibition overcomes multiple resistance mechanisms to selective RAF inhibitors. Mol. Cancer Ther. 14(12), 2700-2711 (2015).

    2. Rasco, D.W., Olszanski, A.J., Patnaik, A., et al. MLN2480, an investigational oral pan-RAF kinase inhibitor, in patients (pts) with relapsed or refractory solid tumors: Phase I study. J. Clin. Oncol. 31(suppl 15), (2013).

    3. Cunniff, E.G.C., Zhang, J., Chouitar, J., et al. Use of combination treatment with the investigational RAF kinase inhibitor MLN2480 and the investigational MEK kinase inhibitor TAK-733 on the growth of BRAF-mutant and RAS-mutant preclinical models of melanoma and CRC. J. Clin. Oncol. 31(15 Suppl), (2013).