aladdin 阿拉丁 B407813 毕卡鲁胺 90357-06-5 10mM in DMSO

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