A highly selective inhibitor of MEK1/2
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AZD 6244

Item No. 11599

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(4-bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
CAS Number
606143-52-6
Synonyms
  • ARRY-142886
  • CL 1,040
  • NSC 741O78
  • Selumetinib
Molecular Formula
C17H15BrClFN4O3
Formula Weight
457.7
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 15 mg/mlDMSO: 20 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
214, 258 nm
SMILES
CN(C=N1)C2=C1C(F)=C(NC3=CC=C(Br)C=C3Cl)C(C(NOCCO)=O)=C2
InChi Code
InChI=1S/C17H15BrClFN4O3/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
CYOHGALHFOKKQC-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $36

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    25 mg

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    50 mg

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    100 mg

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    Product Description

    MEK kinases are central components of diverse intracellular signaling pathways. MEK1 and MEK2 specifically act downstream of growth factor receptors and the proto-oncogenes Ras and Raf to activate ERK1 and ERK2, often leading to an increase in cell proliferation.1 AZD 6244 is a potent, highly selective inhibitor of MEK1 and MEK2 (IC50 = 14 and 530 nM, respectively).2,3,1 It weakly inhibits the EGF receptor (IC50 = 7.0 µM) and has no effect on a large panel of other kinases.2 AZD 6244 suppresses the growth of tumors displaying high levels of phosphorylated MEK1/2 or ERK1/2.3,1 In addition to suppressing growth, it induces apoptosis and differentiation within tumors.4 AZD 6244 has potential, alone or in combination therapy, for promoting tumor regression in various forms of cancer, including those involving mutations of the proto-oncogenes Ras and Raf.5,6

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Yeh, T.C., Marsh, V., Bernat, B.A., et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase ½ inhibitor. Clin. Cancer Res. 13(5), 1576-1583 (2007).

    2. Davis, M.I., Hunt, J.P., Herrgard, S., et al. Comprehensive analysis of kinase inhibitor selectivity. Nat. Biotechnol. 29(11), 1046-1051 (2011).

    3. Huynh, H., Soo, K.C., Chow, P.K.H., et al. Targeted inhibition of the extracellular signal-regulated kinase kinase pathway with AZD6244 (ARRY-142886) in the treatment of hepatocellular carcinoma. Mol. Cancer Ther. 6(1), 138-146 (2007).

    4. Davies, B.R., Logie, A., McKay, J.S., et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase ½ kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models. Mol. Cancer Ther. 6(8), 2209-2219 (2007).

    5. Corcoran, R.B., Cheng, K.A., Hata, A.N., et al. Synthetic lethal interaction of combined BCL-XL and MEK inhibition promotes tumor regressions in KRAS mutant cancer models. Cancer Cell 23(1), 121-128 (2013).

    6. Robert, C., Dummer, R., Gutzmer, R., et al. Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: A phase 2 double-blind randomised study. Lancet Oncol. 14(8), 733-740 (2013).