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抑制剂 > 癌症生物学 > VPC-14449
产品名称:
VPC-14449
型号:
CS-01Y78244
生产地址
国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

10mM*1 mL in DMSO 5 mg 10 mg

CAS

1621375-32-3

别名

N/A

化学名

N/A

分子式

C10H10Br2N4OS

分子量

394.09

溶解度

DMSO : 125 mg/mL (317.19 mM; Need ultrasonic)

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

VPC-14449 is a potent and selective inhibitor of the DNA-binding domain of the androgen receptor (AR-DBD), with IC50 of 0.34 μM for full-length human AR. VPC-14449 reduces the ability of full-length AR as well as AR variants to interact with chromatin. VPC-14449 can be used for the research of prostate cancer[1][2].

VPC-14449 (0.01-100 μM; 24 h) inhibits AR-transcriptional activity and cell viability in LNCaP, C4-2, MR49F, and 22Rv1 cells[2].VPC-14449 (0.01-100 μM; 24 h) dose-dependently inhibits the transiently expressed full-length human AR in PC3 cells (IC50=0.34 μM) without affecting AR protein expression[1].

VPC-14449 (100 mg/kg; i.p. twice daily for 4 weeks) reduces tumor volume and abolishes PSA production with no decrease in body weight over a total duration 4 weeks in LNCaP xenograft model[1].

[1]. Dalal K, et, al. Selectively targeting the DNA-binding domain of the androgen receptor as a prospective therapy for prostate cancer. J Biol Chem. 2014 Sep 19;289(38):26417-26429.

[2]. Dalal K, et, al. Bypassing Drug Resistance Mechanisms of Prostate Cancer with Small Molecules that Target Androgen Receptor-Chromatin Interactions. Mol Cancer Ther. 2017 Oct;16(10):2281-2291.

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:VPC-14449 

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