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Chromatin/Epigenetic Epigenetic Reader Domain ARV-771

ARV-771

Catalog No. T5435   CAS 1949837-12-0

ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively[1].

ARV-771, CAS 1949837-12-0
Pack Size Availability Price/USD Quantity
1 mg In stock 159.00
5 mg In stock 376.00
10 mg In stock 512.00
1 mL * 10 mM (in DMSO) In stock 510.00
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Biological Description
Chemical Properties
Storage & Solubility Information
Description ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34, 4.7, 8.3, 7.6, 9.6, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively[1].
Targets&IC50 BET,  
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[1].
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[1].
Molecular Weight 986.64
Formula C49H60ClN9O7S2
CAS No. 1949837-12-0

Storage

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

Solubility Information

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Citations

References and Literature
1. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 201. Jun 28;113(26):7124-9.

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