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

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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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Size Price Stock Quantity
10 mM * 1 mL $72 In-stock
5 mg $65 In-stock
10 mg $88 In-stock
50 mg $150 In-stock
100 mg $250 In-stock
200 mg $350 In-stock
500 mg $450 In-stock
1 g $650 In-stock
2 g $940 In-stock
5 g $1730 In-stock
10 g Get quote
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Size Price Stock Quantity
10 mM * 1 mL €71 In-stock
5 mg €64 In-stock
10 mg €86 In-stock
50 mg €147 In-stock
100 mg €245 In-stock
200 mg €343 In-stock
500 mg €441 In-stock
1 g €637 In-stock
2 g €921 In-stock
5 g €1695 In-stock
10 g Get quote
50 g Get quote

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Enzalutamide Data Sheet

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    Purity: 99.52%

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    DataSheet

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Related Compound Libraries

Inhibitor Kit

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].

Chemical Information

M.Wt 464.44 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C21H16F4N4O2S
CAS No 915087-33-1
Solvent & Solubility

DMSO ≥90mg/mL Water <1.2mg/mL Ethanol ≥15mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 2.1531 mL 10.7657 mL 21.5313 mL
5 mM 0.4306 mL 2.1531 mL 4.3063 mL
10 mM 0.2153 mL 1.0766 mL 2.1531 mL

Clinical Information of Enzalutamide

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Enzalutamide Astellas Pharma Global Development Inc Hormone refractory prostate cancer 30-SEP-13 30-JUN-18 Phase 4 12-NOV-13
Dendreon Corp Metastatic prostate cancer 30-SEP-13 Phase 2 20-NOV-13
Medivation Inc; Novotech Clinical Research (M) Sdn. Bhd Hormone refractory prostate cancer 30-SEP-10 Phase 3 19-NOV-13
Medivation Inc Hormone refractory prostate cancer 30-SEP-09 30-NOV-12 Phase 3 01-OCT-13
Alliance for Clinical Trials in Oncology Hormone refractory prostate cancer 31-DEC-13 01-DEC-19 Phase 3 27-SEP-13

References on Enzalutamide

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