A MEK inhibitor
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RO4987655

Item No. 19488

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-N-(2-hydroxyethoxy)-5-[(tetrahydro-3-oxo-2H-1,2-oxazin-2-yl)methyl]-benzamide
CAS Number
874101-00-5
Synonyms
  • CH4987655
Molecular Formula
C20H19F3IN3O5
Formula Weight
565.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 10 mg/ml
λmax
280 nm
SMILES
O=C1CCCON1CC2=C(F)C(F)=C(NC3=CC=C(I)C=C3F)C(C(NOCCO)=O)=C2
InChi Code
InChI=1S/C20H19F3IN3O5/c21-14-9-12(24)3-4-15(14)25-19-13(20(30)26-31-7-5-28)8-11(17(22)18(19)23)10-27-16(29)2-1-6-32-27/h3-4,8-9,25,28H,1-2,5-7,10H2,(H,26,30)
InChi Key
FIMYFEGKMOCQKT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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Certificates of Analysis & Batch Specific Data

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    1 mg

    $65

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    5 mg

    $195

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    10 mg

    $293

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    25 mg

    $568

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    Product Description

    RO4987655 is a MEK inhibitor (IC50 = 5 nM).1 It is selective for MEK over 400 kinases at 10 µM. It inhibits proliferation of COLO 205, HT-29, QG56, MIA PaCa-2, and C32 cells with IC50 values of 0.86, 1.7, 9.5, 3.3, and 8.4 nM, respectively. RO4987655 reduces tumor growth in a variety of mouse xenograft models and inhibits the phosphorylation of ERK in tumor tissue in an HT-29 mouse xenograft model when administered at a dose of 6.25 mg/kg per day. It acts synergistically with the mTOR inhibitor everolimus (Item No. 11597) to reduce tumor volume in an HCT116 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Isshiki, Y., Kohchi, Y., Iikura, H., et al. Design and synthesis of novel allosteric MEK inhibitor CH4987655 as an orally available anticancer agent. Bioorg. Med. Chem. Lett. 21(6), 1795-1801 (2011).