An allosteric inhibitor of MEK1/2
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Refametinib

Item No. 16997

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]-6-methoxyphenyl]-1-[(2S)-2,3-dihydroxypropyl]-cyclopropanesulfonamide
CAS Number
923032-37-5
Synonyms
  • BAY 86-9766
  • RDEA119
Molecular Formula
C19H20F3IN2O5S
Formula Weight
572.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 1 mg/mlEthanol: 20 mg/mlEthanol:PBS(pH 7.2) (1:5): 0.1 mg/ml
λmax
275, 299 nm
SMILES
FC1=CC(OC)=C(NS(C2(CC2)C[C@H](O)CO)(=O)=O)C(NC3=CC=C(I)C=C3F)=C1F
InChi Code
InChI=1S/C19H20F3IN2O5S/c1-30-15-7-13(21)16(22)18(24-14-3-2-10(23)6-12(14)20)17(15)25-31(28,29)19(4-5-19)8-11(27)9-26/h2-3,6-7,11,24-27H,4-5,8-9H2,1H3/t11-/m0/s1
InChi Key
RDSACQWTXKSHJT-NSHDSACASA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

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    10 mg

    $183

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    50 mg

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    Product Description

    Refametinib is an allosteric, selective inhibitor of MEK1 and MEK2 (IC50s = 19 and 47 nM, respectively).1 It blocks phosphorylation of ERK1/2 across several human cancer cell lines differing in tissue origin and BRAF mutational status (EC50s = 2.5-16 nM), inhibiting cell cycling in cancer cells but not in primary cells.1 Refametinib is orally available and active in human tumor xenograft models.1 It has potential utility, particularly in combination therapy, in certain forms of cancer.2,3,4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Iverson, C., Larson, G., Lai, C., et al. RDEA119/BAY 869766: A potent, selective, allosteric inhibitor of MEK1/2 for the treatment of cancer. Cancer Res. 69(17), 6839-6847 (2009).

    2. Diep, C.H., Munoz, R.M., Choudhary, A., et al. Synergistic effect between erlotinib and MEK inhibitors in KRAS wild-type human pancreatic cancer cells. Clin. Cancer Res. 17(9), 2744-2756 (2011).

    3. Schmieder, R., Puehler, F., Neuhaus, R., et al. Allosteric MEK1/2 inhibitor refametinib (BAY 86-9766) in combination with sorafenib exhibits antitumor activity in preclinical murine and rat models of hepatocellular carcinoma. Neoplasia 15(10), 1161-1171 (2013).

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