化合物ARV-771 T5435

Product Introduction
Bioactivity


英文名: ARV-771

描述: ARV-771 是基于 PROTAC 技术的有效 BET 降解剂，对 BRD2(1)、BRD2(2)、BRD3(1)、BRD3(2)、BRD4 (1) 和 BRD4(2)的 Kd 分别为 34、4.7、8.3、7.6、9.6 和 7.6 nM。

体外活性: ARV-771, a small-molecule pan-BET degrader based on proteolysis-targeting chimera (PROTAC) technology, demonstrates dramatically improved efficacy in cellular models of CRPC as compared with BET inhibition. ARV-771 effectively degrades BRD2/3/4 in 22Rv1 cells with a DC50 less than 5 nM. c-MYC protein is a downstream effector of BET proteins. Treatment with ARV-771 results in depletion of c-MYC with an IC50 of less than 1 nM. ARV-771 shows strong antiproliferative effect on 22Rv1, VCaP, and LnCaP95 cell lines. ARV-771 treatment has a pronounced effect on cell morphology consistent with apoptosis. FL-AR and AR-V7 mRNA are down-regulated upon treatment with 10 nM ARV-771 in VCaP cells. ARV-771 has an antiandrogenic effect on a number of AR-regulated genes in VCaP cells[1].

体内活性: Treatment of non castrated male Nu/Nu mice bearing AR-V7+ 22Rv1 tumor xenografts with daily subcutaneous injections of ARV-771 at 10 mg/kg for 3 d leads to 37% and 76% down-regulation of BRD4 and c-MYC levels, respectively, in tumor tissue. A marked down-regulation in levels of AR-V7 is observed in the 22Rv1 tumors after ARV-771 treatment[1].

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

溶解度: DMSO : 10 mM


关键字: Epigenetic Reader Domain | ARV-771 | inhibit | ARV771 | PROTACs | Inhibitor | ARV 771

相关产品: MS7972 | CTB | PF-CBP1 | GSK9311 | SF2523 | ZL0420 | Pocenbrodib | GNE-375 | Trotabresib | GSK-5959

相关库: Preclinical Compound Library

化合物ARV-771 T5435信息由TargetMol中国为您提供，如您想了解更多关于化合物ARV-771 T5435报价、型号、参数等信息，欢迎来电或留言咨询。

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