比卡鲁胺 T0380

Product Introduction
Bioactivity


英文名: Bicalutamide

描述: Bicalutamide (ICI-176334) 是一种具有口服活性的非甾体雄激素受体拮抗剂，可研究前列腺癌。

细胞实验: Exponentially growing C4-2 cells are plated into two 96-well plates and incubated overnight at 37 ?C. Twenty-four hours later one plate is aspirated and stored at -80 ?C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37 ?C, the plates are assessed simultaneously for cell growth using the Cy qUANT Cell Proliferation Assay kit. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture.(Only for Reference)

激酶实验: Whole-cell competitive binding assays: Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with 18F-FDHT, increasing concentrations (1pM to 1 μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of 18F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.

体内活性: Bicalutamide在规定的次最大剂量下可将肿瘤生长速率降低79%。Ridaforolimus与bicalutamide联合使用展示出更加有效的抗肿瘤活性。该联合疗法亦具有良好的耐受性，治疗过程中体重无显著变化。在接受联合治疗的小鼠中，血浆PSA水平与肿瘤生长紧密相关。[3]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 60 mg/mL (139.41 mM)
Ethanol : 4.3 mg/mL (10 mM)


关键字: Androgen Receptor | cancer | Bicalutamide | androgen | castration-resistant | ICI 176334 | receptor | prostate cancer | Inhibitor | prostate | inhibit | Autophagy | ICI176334 | anti-androgen | non-steroidal

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相关库: Drug Repurposing Compound Library | Anti-Cancer Drug Library | Clinical Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Nuclear Receptor Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途