An inhibitor of mutant B-Raf kinase
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Encorafenib

Item No. 16994

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1S)-2-[[4-[3-[5-chloro-2-fluoro-3-[(methylsulfonyl)amino]phenyl]-1-(1-methylethyl)-1H-pyrazol-4-yl]-2-pyrimidinyl]amino]-1-carbamic acid, methyl ester
CAS Number
1269440-17-6
Synonyms
  • LGX818
Molecular Formula
C22H27ClFN7O4S
Formula Weight
540.0
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS(pH 7.2)(1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 15 mg/ml
SMILES
O=C(OC)N[C@@H](C)CNC1=NC(C2=CN(C(C)C)N=C2C3=CC(Cl)=CC(NS(C)(=O)=O)=C3F)=CC=N1
InChi Code
InChI=1S/C22H27ClFN7O4S/c1-12(2)31-11-16(17-6-7-25-21(28-17)26-10-13(3)27-22(32)35-4)20(29-31)15-8-14(23)9-18(19(15)24)30-36(5,33)34/h6-9,11-13,30H,10H2,1-5H3,(H,27,32)(H,25,26,28)/t13-/m0/s1
InChi Key
CMJCXYNUCSMDBY-ZDUSSCGKSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $41

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    1 mg

    $77

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    5 mg

    $180

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    Product Description

    Encorafenib is a selective inhibitor of B-RafV600E mutant melanoma cell proliferation (EC50 = 4 nM) with little activity against wild-type B-Raf or a panel of 100 other kinases (IC50s = 900 nM).1 At oral doses of 6 mg/kg in human melanoma xenograft models, encorafenib was shown to decrease phosphorylation of the B-Raf substrate MEK.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Stuart, D.D., Li, N., Poon, D.J., et al. Preclinical profile of LGX818: A potent and selective RAF kinase inhibitor. Cancer Res. 72, (2012).

    2. Huang, T., Karsy, M., Zhuge, J., et al. B-Raf and the inhibitors: From bench to bedside. J. Hematol. Oncol. 6, 1-9 (2013).