MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Enzalutamide

CAS No. : 915087-33-1

MCE 站：Enzalutamide

产品活性：Enzalutamide (MDV3100) 是一种雄激素受体 (androgen receptor (AR)) 拮抗剂，在 LNCaP 前列腺细胞中抑制 AR 的 IC₅₀ 值为 36 nM。Enzalutamide 是一种自噬 (autophagy) 激活剂。

研究领域：Others  |  Autophagy

作用靶点：Androgen Receptor  |  Autophagy

In Vitro: Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 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 inhibits 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 (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg.
Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg.

相关产品：Drug Repurposing Compound Library Plus  |  FDA-Approved Drug Library Plus  |  FDA-Approved Drug Library Mini  |  Bioactive Compound Library Plus  |  FDA-Approved Drug Library  |  Anti-Cancer Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Drug Repurposing Compound Library  |  Orally Active Compound Library  |  FDA Approved & Pharmacopeial Drug Library  |  Targeted Therapy Drug Library   |  DHEA  |  Medroxyprogesterone acetate  |  Bicalutamide  |  Flutamide  |  Spironolactone  |  Danazol  |  Testosterone propionate  |  Dimethylcurcumin  |  Epiandrosterone  |  Ailanthone  |  3,3'-Diindolylmethane  |  Clascoterone  |  Lupeol  |  Nilutamide  |  Cyproterone acetate  |  YK11  |  Stanolone benzoate  |  Triptophenolide  |  EPI-001  |  Adrenosterone  |  Dehydroisoandrosterone 3-acetate  |  PROTAC AR Degrader-4 TFA  |  11-Ketodihydrotestosterone  |  Boldenone Undecylenate  |  D4-abiraterone  |  Isosilybin B  |  Prochloraz  |  RU 58841  |  2,2,5,7,8-Pentamethyl-6-Chromanol

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。