中文名：毕卡鲁胺
英文名：Bicalutamide (ICI-176334)
英文别名：N-[4-cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methyl-propanamide
纯度：10mM in DMSO
货号：B407813
包装：1ml
Cas号：90357-06-5
存储温度：-80℃储存
产品介绍：
Information
Bicalutamide (ICI-176334) Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy .
In vitro
Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone.
In vivo
Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice.
Cell Data
cell lines：
Concentrations：0-1 μM
Incubation Time：72 hours
Powder Purity:≥99%
查看阿拉丁官网此产品相关对应页面：https://www.aladdin-e.com/zh_cn/B407813.html
关键字： N-?[4-?cyano-?3-?(trifluoromethyl)?phenyl]?-?3-?[(4-?fluorophenyl)?sulfonyl]?-?2-?hydroxy-?2-?methyl-propanamide
上海阿拉丁生化科技股份有限公司是A股上市公司（（股票代码：688179），专注于科研试剂的研发、生产和销售，已陆续建立多个工厂和研发中心。作为领军企业，阿拉丁始终坚持质量第一，连续13年被评为“最受欢迎试剂品牌”。
阿拉丁目前常备库存试剂产品品种超过7万种，SKU总数超过46万，产品线涵盖了化学试剂、生化试剂、药靶配体、蛋白质和抗体等多个领域，是国内少数化学试剂到生物试剂全面发展的国产试剂品牌，产品同步发布在我们国内（www.aladdin-e.com）和海外（www.aladdinsci.com）电商平台。