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ARV-771

CAS No. : 1949837-12-0

MCE 国际站：ARV-771

产品活性：ARV-771 是一种基于von Hippel-LindauE3连接酶的有效 BET PROTAC。对 BRD2(1)，BRD2(2)，BRD3(1)，BRD3(2)，BRD4(1) 和 BRD4(2) 的 K_d 值分别为 34 nM，4.7 nM，8.3 nM，7.6 nM，9.6 nM 和 7.6 nM。

研究领域：PROTAC  |  Epigenetics

作用靶点：PROTACs  |  Epigenetic Reader Domain

In Vitro: 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 potently 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.

In Vivo: 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 results in 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.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Histone Modification Research Compound Library  |  Anti-Cancer Compound Library  |  Reprogramming Compound Library  |  Anti-Blood Cancer Compound Library  |  Heterocyclic Compound Library  |  PROTAC Library  |  BRD4 Inhibitor-18  |  LC-2  |  ACBI2  |  iRucaparib-AP6  |  BI01826025  |  Curcumin  |  BSJ-04-132  |  GSK6853  |  MI-1  |  PROTAC VEGFR-2 degrader-1  |  SR-1114  |  GSK 4027  |  ZL0590  |  PROTAC CRABP-II Degrader-3  |  PROTAC Sirt2 Degrader-1  |  CRBN-6-5-5-VHL  |  BRD4 Inhibitor-26  |  Apabetalone  |  PROTAC BRD2/BRD4 degrader-1  |  MS645  |  OF-1  |  I-CBP112  |  BRM/BRG1 ATP Inhibitor-2  |  PROTAC CDK9 degrader-8  |  BSJ-03-204  |  UMB-32  |  JPS016  |  Ziftomenib  |  GSK761  |  XX-650-23

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