A potent MEK inhibitor
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CI-1040

Item No. 11580

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[(2-chloro-4-iodophenyl)amino]-N-(cyclopropylmethoxy)-3,4-difluoro-benzamide
CAS Number
212631-79-3
Synonyms
  • PD 184352
Molecular Formula
C17H14ClF2IN2O2
Formula Weight
478.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlEthanol: 2 mg/ml
λmax
281, 312 nm
SMILES
FC1=CC=C(C(NOCC2CC2)=O)C(NC3=C(Cl)C=C(I)C=C3)=C1F
InChi Code
InChI=1S/C17H14ClF2IN2O2/c18-12-7-10(21)3-6-14(12)22-16-11(4-5-13(19)15(16)20)17(24)23-25-8-9-1-2-9/h3-7,9,22H,1-2,8H2,(H,23,24)
InChi Key
GFMMXOIFOQCCGU-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $90

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    10 mg

    $158

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    25 mg

    $349

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    50 mg

    $653

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    Product Description

    CI-1040 is a benzhydroxamate compound that potently inhibits MEK in an in vitro mitogen-activated protein kinase cascade assay with an IC50 value of 2.3 nM (Kd = 74 nM when activated with adenosine triphosphate).1,2 It can suppress phosphorylation of ERK in mouse colon 26 tumors with an IC50 value of 35 nM and demonstrates in vivo activity with oral administration in a mouse tumor model.1 The second-generation MEK inhibitor PD 0325901 (Item No. 13034) is a structural derivative of CI-1040 that was developed for improved solubility.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Barret, S.D., Bridges, A.J., Dudley, D.T., et al. The discovery of the benzhydroxamate MEK inhibitors CI-1040 and PD 0325901. Bioorg. Med. Chem. Lett. 18, 6501-6504 (2008).

    2. VanScyoc, W.S., Holdgate, G.A., Sullivan, J.E., et al. Enzyme kinetics and binding studies on inhibitors of MEK protein kinase. Biochemistry 47, 5017-5027 (2008).