Description
Enzalutamide (MDV3100) is an antagonist of androgen-receptor (AR) with IC50 of 36 nM.
Product Overview
MDV3100, known as Enzalutamide, is a second-generation androgen receptor (AR) signaling inhibitor. It has been demonstrated impressive affinity to the AR compared to the first-generation AR inhibitors. It is able to inhibit binding of androgens to the AR, AR nuclear translocation, and the association of the AR with DNA. The AR is a 919-amino acid member of the steroid receptor transcription factor superfamily with different domains including an N-terminal regulation domain, a central DNA binding domain, and a C-terminal domain, which includes the ligand-binding domain incorporated within its protein structure. MDV3100 was identified by the Sawyers/Jung laboratories by using the nonsteroidal agonist. Testing was showing that it induced apoptosis in VCaP cells, an AR gene amplified human prostate cancer line, while bicalutamide was ineffective.
Synonyms
Enzalutamide, MDV3100, MDV-3100, MDV 3100
Targets
Androgen-receptor
Molecular Formula
C21H16F4N4O2S
Chemical Name
4-[3-[4-cyano-3-(trifluoromethyl)phenyl]-5,5-dimethyl-4-oxo-2-sulfanylideneimidazolidin-1-yl]-2-fluoro-N-methylbenzamide
Solubility
Soluble in DMSO > 10 mM
Shipping Conditions
Evaluation sample solution: ship with blue ice. All other available size: ship with RT, or blue ice upon request
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