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Cat. No. Name Size Price Add Cart
KI1330AZD624450 mg$144
AZD6244100 mg$208
AZD6244200 mg$272
AZD6244500 mg$592

Chemical Characteristic

Product NameAZD6244
SynonymsSelumetinib, ARRY-142886
CAS No.606143-52-6
Molecular Weight 457.69
FormulaC17H15BrClFN4O3
Chemical Name5-[(4-Bromo-2-chlorophenyl)amino]-4-fluoro-N-(2-hydroxyethoxy)-1-methyl-1H-benzimidazole-6-carboxamide
Smilesc1nc2c(n1C)cc(c(c2F)Nc1c(cc(cc1)Br)Cl)C(=O)NOCCO
Chemical Structure

Biological activities

AZD6244 is a potent, selective, and ATP-uncompetitive inhibitor of MEK1/2 kinases. The IC50 of AZD6244 is 14 nM against purified constitutively active MEK1. The IC50 values against Raf-activated MEK1 and MEK2 are similar. In contrast, AZD6244 prevents HT-29, Malme-3M, and SK-MEL-28 cell lines with IC50 of 175, 59 and 93 nM, respectively.[1] AZD6244 inhibits Colo-205 cells and Calu-6 cells with IC50 of 30 nM and 0.7 µM, respectively.[2] In two-dimensional cell culture, AZD6244 is cytostatic and decreases the growth of melanoma cells in a concentration-dependent fashion through the induction of G1-phase cell cycle arrest.[3] AZD6244 results in growth inhibition, elevation of the cleavage of caspase-3 and caspase-7, and cleaves poly(ADP)ribose polymerase, but inhibition of ERK1/2 and p90RSK phosphorylation in primary HCC cells.[4] AZD6244 inhibits the growth of several cell lines containing B-Raf and Ras mutations but has no effect on a normal fibroblast cell line. When dosed orally, AZD6244 prevents both ERK1/2 phosphorylation and growth of HT-29 xenograft tumors in nude mice, as well as a BxPC3 xenograft model.[1] When dosing is commenced at a mean tumor size of 0.2 cm3, chronic dosing with 25 mg/kg bd AZD6244 completely inhibits growth of Colo-205 tumors. AZD6244 inhibits partial growth of SW-620 xenografts by 73%. AZD6244 causes apoptosis in Colo-205 xenografts. An acute dose of 25 mg/kg AZD6244 results in a reduction in cytoplasmic and nuclear p-ERK in Colo-205 xenografts.[2] AZD6244 downregulates phospho-ERK in the tumors and significantly suppressed tumor growth.[3] AZD6244 results in a dose-dependent inhibition of tumor growth when given p.o. to mice bearing HCC xenografts.[4]

Protocols

In vivo: AZD6244 is dissolved in a methocel/polysorbate buffer.[2]

References

[1] Yeh TC, et al. Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor. Clin Cancer Res. 2007, 13(5): 1576-1583.
[2] Davies BR, et al. AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models.Mol Cancer Ther. 2007, 6(8): 2209-2219.
[3] Haass NK, et al. The mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor AZD6244 (ARRY-142886) induces growth arrest in melanoma cells and tumor regression when combined with docetaxel.Clin Cancer Res. 2008, 14(1): 230-239.
[4] Huynh 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. 2007, 6(1): 138-146.

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