型号:
产品价格:电议      采购度:1312      原产地:美洲
发布时间:2022/1/21 22:32:04 所属地区:国外 国外
简要描述:
Bavdegalutamide (ARV-110) 是一种具有口服活性的,特异性的雄激素受体 (AR) PROTAC 类降解剂。Bavdegalutamide 能促进 AR 的泛素化和降解,可用于前列腺癌的研究。
标签:ARV-110
产品详情
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。
CAS No. : 2222112-77-6
MCE 站:Bavdegalutamide
产品活性:Bavdegalutamide (ARV-110) 是一种具有口服活性的,特异性的雄激素受体 (AR) PROTAC 类降解剂。Bavdegalutamide 能促进 AR 的泛素化和降解,可用于前列腺癌的研究。
研究领域:Others
作用靶点:Androgen Receptor
In Vitro: Bavdegalutamide completely degrades AR in all cell lines tested, with an observed 50% degradation concentration (DC50) < 1 nM.
Bavdegalutamide (0.01 nM-300 nM) leads to AR degradation in LNCaP cells in a dose-dependent manner.Bavdegalutamide (10 nM; 0.5-24 hours) leads to AR degradation in VCaP cells in a time-dependent manner.Bavdegalutamide (10-1000 nM) suppresses the expression of the AR-target gene PSA, inhibits AR-dependent cell proliferation, and induces apoptosis at low nanomolar concentrations.Bavdegalutamide (0.01 nM-100 nM) degrades clinically relevant mutant AR proteins (WT AR, F876L, T877A, M896V and H874V), and retains activity in a high androgen environment (R1881, 100 nM) in VCaP cells.
In Vivo: Bavdegalutamide (oral gavage; 1 mg/kg; QD) exhibits a greater than 90% AR degradation in vivo. In LNCaP, VCaP and prostate cancer patient derived xenograft (PDX) models, Bavdegalutamide also exhibits significant inhibition of tumor growth and AR signaling.Bavdegalutamide (oral gavage; 3 or 10 mpk; 30 days) demonstrates in vivo efficacy and reduction of AR-target gene expression in a long term, castrate, enzalutamide-resistant VCaP tumor model. The TGI are 70% and 60% for 3 mpk and 10 mpk dosage. Respectively.
相关产品:Drug Repurposing Compound Library Plus | Clinical Compound Library Plus | Bioactive Compound Library Plus | Anti-Cancer Compound Library | Clinical Compound Library | Drug Repurposing Compound Library | Orally Active Compound Library | Transcription Factor Targeted Library | Enzalutamide | DHEA | Apalutamide | Medroxyprogesterone acetate | Testosterone propionate | Bicalutamide | Darolutamide | Spironolactone | Flutamide | Danazol | Dimethylcurcumin | Proxalutamide | ARCC-4 | AZD3514 | BMS-564929 | Ailanthone | ARD-266 | Lupeol | 3,3'-Diindolylmethane | ACP-105 | GSK-2881078 | LY2452473 | Nilutamide | EPI-001 | Epiandrosterone | GLPG0492 | UT-155 | Vosilasarm | Clascoterone
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 染料试剂 | PROTAC | 同位素标记物
Trending products:Recombinant Proteins | Bioactive Screening Libraries | Natural Products | Dye Reagents | PROTAC | Isotope-Labeled Compounds
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。
更新时间:2024/1/2 10:19:52
留言咨询
温馨提示
1.遵守中华人民共和国有关法律、法规,尊重网上道德,承担一切因您的行为而直接或间接引起的法律责任。
2.请您真实的反映产品的情况,不要捏造、诬蔑、造谣。如对产品有任何疑问,也可以留言咨询。
3.未经本站同意,任何人不得利用本留言簿发布个人或团体的具有广告性质的信息或类似言论。
相关新闻
相关产品