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MDV3100 (Enzalutamide) | AR antagonist

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Catalog #:

Product Description

MDV3100 (Enzalutamide) is an orally-available thioxoimidazoline androgen receptor antagonist approved in August, 2012, for the treatment of castration-resistant prostate cancer (CRPC). In LNCaP/AR cells, MDV3100 has a potency of 36 nM. [1] MDV3100 blocks testosterone binding to AR and has approximately 5-fold higher binding affinity for AR than bicalutamide. In contrast to bicalutamide, MDV3100 does not promote translocation of AR to the nucleus and also prevents AR binding to DNA and other coactivator proteins. In contrast to bicalutamide in LNCaP cell lines, MDV3100 downregulates expression of PSA and TMPRSS2 genes and is an antagonist of the W741C mutant androgen receptor.

Early preclinical studies also indicate that MDV3100 may be a potential treatment for breast cancer; enrollment for Phase I trials are underway.

Technical information:

Chemical Formula:   C21H16F4N4O2S
CAS #:   915087-33-1
Molecular Weight:   464.44
Purity:   >99%
Appearance:   White
Chemical Name:   4-(3-(4-cyano-3-(trifluoromethyl)phenyl)-5,5-dimethyl-4-oxo-2-thioxoimidazolidin-1-yl)-2-fluoro-N-methylbenzamide
Solubility:   Up to 100 mM in DMSO
Synonyms:   Enzalutamide, MDV-3100, MDV 3100, MDV3100

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


1. Tran et al., Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science 2009, 324 (5928), 787-790 Pubmed ID: 19359544
2. http://en.wikipedia.org/wiki/Enzalutamide

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

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