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Selumetinib
$79 – $515
Products Details
Product Description
– Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
Web ID
– HY-50706
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C17H15BrClFN4O3
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]Garon EB, et al. Identification of common predictive markers of in vitro response to the Mek inhibitor selumetinib (AZD6244; ARRY-142886) in human breast cancer and non-small cell lung cancer cell lines. Mol Cancer Thera, 2010, 9 (7), 1985-1994.|[3]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 Therapy, 2007, 6 (1), 138-146|[4]Sebolt-Leopold JS, et al. Targeting the mitogen-activated protein kinase cascade to treat cancer. Nat Rev Cancer. 2004 Dec;4(12):937-47.|[5]Dela Cruz FS, et al. A case study of an integrative genomic and experimental therapeutic approach for rare tumors: identification of vulnerabilities in a pediatric poorly differentiated carcinoma. Genome Med. 2016 Oct 31;8(1):116.|[6]Weisberg E, et al. Upregulation of IGF1R by mutant RAS in leukemia and potentiation of RAS signaling inhibitors by small-molecule inhibition of IGF1R. Clin Cancer Res. 2014 Nov 1;20(21):5483-95.
CAS Number
– 606143-52-6
Molecular Weight
– 457.68
Compound Purity
– 99.87
SMILES
– O=C(C1=C(C(F)=C2N=CN(C2=C1)C)NC3=CC=C(C=C3Cl)Br)NOCCO
Clinical Information
– Launched
Research Area
– Cancer
Solubility
– DMSO : 10 mg/mL (ultrasonic)|DMSO : 20.83 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Apoptosis;MEK
Isoform
– MEK;MEK1;MEK2
Pathway
– Apoptosis;MAPK/ERK Pathway
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
