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Products are for research use only. Not for human use. We do not sell to patients.
(MDV3100; MDV-3100; MDV 3100)
Enzalutamide Chemical Structure
Protease Inhibitor Cocktail
protease inhibitor cocktails are used in mammalian cell lysates or tissue extracts to increase protein stability.
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
IC50 value: 36 nM 
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) . Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex .
in vivo: Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg .
|M.Wt||464.44||Storage||Please store the product under the recommended conditions in the Certificate of Analysis.|
|Solvent & Solubility||
DMSO ≥90mg/mL Water <1.2mg/mL Ethanol ≥15mg/mL
|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|
|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|
CAS No: 1242137-16-1
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