Molecular Weight(MW): 464.44
Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
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|Description||Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.|
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. |
AR reporter assay:Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed.
|In vitro||DMSO||92 mg/mL warmed (198.08 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+1% CMC Na+1% Tween-80
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03207529||Not yet recruiting||Malignant Neoplasm of Breast||M.D. Anderson Cancer Center|Novartis|Astellas Pharma Global Development Inc.||January 2019||Phase 1|
|NCT03700099||Not yet recruiting||Prostate Cancer|Castration-resistant Prostate Cancer||Instituto do Cancer do Estado de São Paulo|Astellas Pharma Inc||December 2018||Phase 2|
|NCT03734653||Not yet recruiting||Prostate Cancer|Castration-Resistant Prostate Cancer||University of Colorado Denver|Cancer League of Colorado Inc||December 2018||Early Phase 1|
|NCT03709550||Not yet recruiting||Castration Levels of Testosterone|Castration-Resistant Prostate Carcinoma|Metastatic Prostate Carcinoma in the Soft Tissue|Prostate Carcinoma Metastatic in the Bone|PSA Level Greater Than or Equal to Two|PSA Progression|Stage IV Prostate Cancer AJCC v8|Stage IVA Prostate Cancer AJCC v8|Stage IVB Prostate Cancer AJCC v8||Roswell Park Cancer Institute|National Cancer Institute (NCI)||November 30 2018||Phase 1|Phase 2|
|NCT03531827||Recruiting||Metastatic Castration Resistant Prostate Cancer|Prostate Neoplasms||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||November 20 2018||Phase 2|
|NCT03478904||Recruiting||Prostate Cancer||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||November 20 2018||Phase 1|
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Frequently Asked Questions
I would like to inquire about the usage or solubility of S1250, Enzalutamide.
For in vivo experiment, S1250 can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5mg/ml as a suspension for oral gavage. And it can be dissolved in 15% DMSO+85% PEG 300 at 10mg/ml as a clear solution. When prepare the solution, please dissolve the compound in DMSO clearly first, then add PEG.