MDV3100 (Enzalutamide)

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Cat No.

CEI-1416

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.

CAS_No

915087-33-1

Molecular Weight

464.4

Purity

0.9912

Storage

Store at -20°C

Synonyms

Enzalutamide, MDV3100, MDV-3100, MDV 3100

Targets

Androgen-receptor

IC50

36 nM

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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Our Products Cannot Be Used As Medicines Directly For Personal Use.

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