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AZD6244 | ERK inhibitor

AZD6244 (606143-52-6) is a potent, selective, and non-ATP competitive inhibitor of MEK1/2 (IC50 MEK1 = 14 nM) and ERK 1/2 phosphorylation (IC50 = 10 nM).1,2 AZD6244 is in clinical trials for treating various cancers.3-7

1) Davies et al. (2007), 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/pharmacodynamics relationship, and potential for combination in preclinical models; Mol. Cancer Ther., 6 2209
2) Yeh et al. (2007), Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor; Clin. Cancer Res., 13 1576
3) Catalanotti et al. (2013), Phase II trial of MEK inhibitor selumetinib(AZD6244) in patients with BRAFV600E/K-mutated melanoma; Clin. Cancer Res., 19 2257
4) O'Neil et al. (2011), Phase II study of the mitogen-activated protein kinase 1/2 inhibitor selumetinib in patients with advanced hepatocellular carcinoma; J. Clin. Oncol., 29 2350
5) Khurum et al. (2012), A phase I dose escalation study of oral MK-2206 (allosteric Akt inhibitor) with oral selumetinib (AZD6244)(MEK 1/2 inhibitor) in patients with advanced or metastatic solid tumors; J. Clin. Oncol., 30 e13599
6) Hainsworth et al. (2010), A phase II, open label, randomized study to assess the efficacy and safety of AZD6244 versus pemetrexed in patients with non-small cell lung cancer who have failed one or two prior chemotherapeutic regimens; J. Thorac. Oncol., 5 1630
7) Bodoky et al. (2012), A phase II open-label randomized study to assess the efficacy and safety of selumetinib (AZD6244) versus capecitabine in patients with advanced or metastatic pancreatic cancer who have failed first-line gemcitabine therapy; Invest. New Drugs, 30 1216

Focus Biomolecules cell signaling reagent supplier, chemical structure of AZD6244 | ERK inhibitor | CAS 606143-53-6

Catalog#  10-4509

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Catalog Number:
ERK inhibitor
Alternate Names:
ARRY-142886, Selumetinib
Molecular Weight:
Molecular Formula:
Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 2 mg/ml)
Physical Properties:
White solid
99% by HPLC
NMR (Conforms)
Storage Temperature:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20° for up to 2 months.
Shipping Code:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

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