Selumetinib
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.
Product Specifications
CAS Number
[606143-52-6]
Product Name Alternative
AZD6244; ARRY-142886
UNSPSC
12352005
Hazard Statement
H302, H315, H319, H335
Target
Apoptosis; MEK
Type
Reference compound
Related Pathways
Apoptosis; MAPK/ERK Pathway
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/Selumetinib.html
Purity
99.87
Solubility
DMSO : 20.83 mg/mL (ultrasonic) |H2O : < 0.1 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
O=C(C1=C(C(F)=C2N=CN(C2=C1)C)NC3=CC=C(C=C3Cl)Br)NOCCO
Molecular Formula
C17H15BrClFN4O3
Molecular Weight
457.68
Precautions
H302, H315, H319, H335
References & Citations
[1]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|[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]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.|[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.
Shipping Conditions
Room Temperature
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Launched
Isoform
MEK; MEK1; MEK2
Citation 01
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