A potent, orally available MEK1 inhibitor
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Cobimetinib

Item No. 19563

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]phenyl][3-hydroxy-3-(2S)-2-piperidinyl-1-azetidinyl]-methanone
CAS Number
934660-93-2
Synonyms
  • GDC-0973
  • RG-7420
  • XL518
Molecular Formula
C21H21F3IN3O2
Formula Weight
531.3
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMSO: 25 mg/mlEthanol: 11 mg/ml
λmax
240, 276 nm
SMILES
FC1=C(NC2=CC=C(I)C=C2F)C(C(N3CC([C@@H]4CCCCN4)(O)C3)=O)=CC=C1F
InChi Code
InChI=1S/C21H21F3IN3O2/c22-14-6-5-13(19(18(14)24)27-16-7-4-12(25)9-15(16)23)20(29)28-10-21(30,11-28)17-3-1-2-8-26-17/h4-7,9,17,26-27,30H,1-3,8,10-11H2/t17-/m0/s1
InChi Key
BSMCAPRUBJMWDF-KRWDZBQOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $54

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    5 mg

    $197

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    10 mg

    $367

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    25 mg

    $783

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    Product Description

    Cobimetinib is a potent, orally available inhibitor of MEK1 (IC50 = 4.2 nM).1,2 It shows more than 100-fold selectivity for MEK when tested against a panel of more than 100 serine-threonine and tyrosine kinases. Cobimetinib induces differentiation and apoptosis in cancer cell lines and is more effective when combined with additional inhibitors, like PLX4032 (Item No. 10618).2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Akinleye, A., Furgan, M., Mukhi, N., et al. MEK and the inhibitors: From bench to bedside. J. Hematol. Oncol. 6, 27 (2013).

    2. Hoeflich, K.P., Merchang, M., Orr, C., et al. Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibition. Cancer Res. 72(1), 210-219 (2012).

    3. Medina, T.M., and Lewis, K.D. The evolution of combined molecular targeted therapies to advance the therapeutic efficacy in melanoma: A highlight of vemurafenib and cobimetinib. Onco Targets Ther. 9, 3739-3752 (2016).

    4. Sing, A., Ruan, Y., Tippett, T., et al. Targeted inhibition of MEK1 by cobimetinib leads to differentiation and apoptosis in neuroblastoma cells. J. Exp. Clin. Cancer Res. 34(1), 104 (2015).