606143-52-6 Selumetinib AKSci X2640
 
 
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  X2640    
Selumetinib
, 98% (HPLC), powder
 
AZD6244




IDENTITY
CAS Number:606143-52-6
MDL Number:MFCD11977472
MF:C17H15BrClFN4O3
MW:457.69
SPECIFICATIONS & PROPERTIES
Purity:98% (HPLC), powder
Spectra:NMR, LCMS, FT-IR, HPLC
Physical Form:White powder
Melting Point:>219°C
Density:1.692
Refractive Index:1.672
Long-Term Storage:Store long-term at -20°C
UN #:Not hazmat

BIOLOGICAL INFO
Application(s):Inhibitor of MEK1

REVIEW

 Selumetinib (AZD6244) is a second-generation, orally available, potent and selective ATP non-competitive inhibitor of MEK 1/2. In direct assays, AZD6244 selectively inhibits purified active MEK1 and MEK2 with an IC50 of 14 nM, and AZD6244 has reported IC50 values of <100nm for MEK1 in ELISA assays and in bindings assays against recombinant domains of MEK2, Kd values were 53nM for AZD6244. AZD6244 demonstrated very effective anti-proliferation effects against several different cell lines with IC50 values ranging from a low of 3nM to < 1 μM depending upon the cell system used, and the compound inhibits basal and growth factor-stimulated phosphorylation of ERK1/ 2 with IC50 concentrations < 40 nM. AZD6244 has demonstrated potent dose-dependent antitumor activity against a panel of mouse xenograft models of colorectal, pancreatic, liver, skin, and lung cancer, and inhibition of tumor growth was found to correlate with the reduction of phospho-ERK1/2 levels in tumors.

GHS

Pictograms

Signal Word
Warning

Hazard Statements
H315; H319; H335

Precautionary Statements
P261; P264; P271; P280; P302+P352; P304+P340; P305+P351+P338; P312; P321; P332+P313; P337+P313; P362; P403+P233; P405; P501


Current as of January 19, 2019


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CATEGORIES

 APIs and Bioactives > Protein Kinase Inhibitors


PubChem