AZD6244 | ERK inhibitor
NMR (Conforms)
Available Options
| Size : | Price | Quantity | |
|---|---|---|---|
| 10 mg | $40.00 | ||
| 50 mg | $85.00 |
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
References/Citations:
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
NMR (Conforms)
Safety Data Sheet:
Product Data Sheet:
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee
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
References/Citations:
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
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