A MEK1/2 inhibitor
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Binimetinib

Item No. 16996

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(4-bromo-2-fluorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
CAS Number
606143-89-9
Synonyms
  • ​ARRY-438162
  • MEK162
Molecular Formula
C17H15BrF2N4O3
Formula Weight
441.2
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/mlEthanol: 0.5 mg/ml
λmax
213, 257 nm
SMILES
BrC1=CC(F)=C(NC2=C(F)C(N=CN3C)=C3C=C2C(NOCCO)=O)C=C1
InChi Code
InChI=1S/C17H15BrF2N4O3/c1-24-8-21-16-13(24)7-10(17(26)23-27-5-4-25)15(14(16)20)22-12-3-2-9(18)6-11(12)19/h2-3,6-8,22,25H,4-5H2,1H3,(H,23,26)
InChi Key
ACWZRVQXLIRSDF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $35

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    10 mg

    $53

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    50 mg

    $123

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    100 mg

    $228

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    Product Description

    Binimetinib is a MEK1 and MEK2 inhibitor (IC50s = 1.8 and 0.92 nM, respectively).1 It is selective for MEK1/2 over a panel of RAF/MEK/ERK pathway kinases at 10 µM. Binimetinib reduces cell growth in HT-29, COLO 205, and LoVo colorectal cancer cell lines (IC50s = 0.48, 0.52, and 2.2 nM, respectively). It reduces tumor volume in a COLO 205 mouse xenograft model when administered at a dose of 0.3 mg/kg. Formulations containing binimetinib have been used in the treatment of various cancers.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yamaguchi, T., Kakefuda, R., Tajima, N., et al. Antitumor activities of JTP-74057 (GSK1120212), a novel MEK1/2 inhibitor, on colorectal cancer cell lines in vitro and in vivo. Int. J. Oncol. 39(1), 23-31 (2011).