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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].

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ARV-771, CAS 1949837-12-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 55.00
5 mg	In stock	$ 122.00
10 mg	In stock	$ 197.00
25 mg	In stock	$ 393.00
50 mg	In stock	$ 586.00
100 mg	In stock	$ 838.00
1 mL * 10 mM (in DMSO)	In stock	$ 213.00

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Purity: 99.69%

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	BRD2(2):4.7 nM (Kd), BRD3(2):7.6 nM (Kd), BRD4(2):7.6 nM (Kd), BRD4(1):9.6 nM (Kd), BRD3(1):8.3 nM (Kd), BRD2(1):34 nM (Kd)
In vitro	ARV-771, utilizing proteolysis-targeting chimera (PROTAC) technology, outperforms BET inhibitors in CRPC cellular models by effectively degrading BRD2/3/4 in 22Rv1 cells with a DC50 of less than 5 nM. This compound also significantly reduces c-MYC protein levels, a key BET protein effector, achieving an IC50 under 1 nM. Demonstrating potent anti-proliferative abilities, ARV-771 impacts 22Rv1, VCaP, and LnCaP95 cell lines, inducing apoptosis and altering cell morphology. Furthermore, treatment with 10 nM of ARV-771 notably suppresses FL-AR and AR-V7 mRNA in VCaP cells and exerts an antiandrogenic influence on several AR-regulated genes within these cells[1].
In vivo	Administering daily subcutaneous injections of ARV-771 at a dosage of 10 mg/kg for three days to non-castrated male Nu/Nu mice with AR-V7+ 22Rv1 tumor xenografts resulted in a significant reduction of BRD4 and c-MYC levels in the tumor tissue by 37% and 76%, respectively. Additionally, a notable decrease in AR-V7 levels was observed in the 22Rv1 tumors following the treatment with ARV-771[1].

Molecular Weight	986.64
Formula	C49H60ClN9O7S2
CAS No.	1949837-12-0

Storage

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

Solubility Information

DMSO: 10 mM

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.

Related compound libraries

This product is contained In the following compound libraries：

Preclinical Compound Library

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Keywords

ARV-771 1949837-12-0 Chromatin/Epigenetic Epigenetic Reader Domain inhibit ARV771 PROTACs Inhibitor ARV 771 inhibitor

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