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Background Information:
AZD6244 (Selumetinib) is a potent, selective and orally available small molecule inhibitor of MEK1/2 with an enzymatic IC50 value of 14 nM against MEK1. Block ERK1/2 phosphorylation with an IC50 value of 10 nM. Display broad antitumor activities in cell lines and in animal models either as a single agent, or in combination with other antitumor agents..
Reference:
1. Yeh, T. C., et al, Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor, Clin Cancer Res. 13(5):1576-83 (2007).
2. Friday, B.B., et al., BRAF V600E disrupts AZD6244-induced abrogation of negative feedback pathways between extracellular signal-regulated kinase and Raf proteins, Cancer Res. 68(15):6145-53 (2008).
3. S. V. Holt, et al., The MEK1/2 inhibitor, Selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft models, British Journal of Cancer (2012) 106, 858–866.
APIM050100: AZD6244 (SELUMETINIB)
CAS No.: 606143-52-6.
Molecular Formula: C17H15BrClFN4O3 ? 0.3H2O.
Molecular Weight: 463.1.
Purity: 99.5% (HPLC).
QC: HPLC-MS, 1HNMR, and Quantitative Elemental Analysis.
Solubility: Soluble in DMSO.
Storage: Store at 0°C (short term), -20°C (long term), desiccated.
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