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Products are for research use only. Not for human use. We do not sell to patients.

Signaling Pathway

Enzalutamide

HY-70002

(MDV3100; MDV-3100; MDV 3100)

Enzalutamide
Enzalutamide Chemical Structure

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.

Price and Availability of Enzalutamide
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Enzalutamide Data Sheet

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Purity: 99.02%

Enzalutamide

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Biological Activity of Enzalutamide

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
IC50 value: 36 nM [1]
Target: androgen-receptor
in vitro: Enzalutamide has greater affinity to AR than Bicalutamide does in a competition assay with 16β-[18F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys) [1]. Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex [2].
in vivo: Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg [1].

Clinical Information of Enzalutamide

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[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790.

[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446.

Products are for research use only. Not for human use. We do not sell to patients.

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