Successful, we will replay to you quickly.OK
Please select the quantity.OK
Your message is being sent, please wait.Close
Send mail failed, please send again!Close
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
17 alpha-propionate(CB-03-01) is a new topical and peripherally selective androgen antagonist.
Andarine (S-4) is an investigational selective androgen receptor modulator (SARM) and an active partial agonist.
ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM, useful for prostate cancer treatment.
ASC-J9(GO-Y025; Dimethylcurcumin), is antitumor agent; ASC-J9 suppresses castration-resistant prostate cancer growth via degradation of full-length and splice variant androgen receptors.
AZD3514 is a potent and oral androgen receptor downregulator with Ki of 2.2 (mu)M and has ability of reducing AR protein expression.
Bicalutamide(Casodex) is an oral non-steroidal anti-androgen for prostate cancer; binds to the androgen receptor.
BMS-564929 is a novel, highly potent, orally active, nonsteroidal tissue selective androgen receptor (AR) modulator (Ki= 2.11 nM).
Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.
Danazol is a derivative of the synthetic steroid ethisterone, that suppresses the production of gonadotrophins, and has some weak androgenic effects.
Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.
Other Countries & RegionsSee Worldwide Distributors