製品番号: HY-100972

Biologically Validated

ARV-771

Name: ARV-771
Brand: MedChemExpress
SKU: HY-100972
Price: 70.00 USD
Availability: InStock
Rating: 5 (30 reviews)

30 Cited Publications

カスタマーレビュー

Based on 30 publication(s) in Google Scholar

ARV-771 is a BET PROTAC degrader, with K_d values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research.
(Pink: BET ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: linker).

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純度 : 99.82%
CAS 番号: 1949837-12-0
分子式: C₄₉H₆₀ClN₉O₇S₂
分子量:986.64

保管条件:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

ARV-771 構造式

CAS 番号: 1949837-12-0

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

生物活性
- 製品説明
- IC₅₀ & Target
- MCE検証データ
- Cellular Effect
- 体外実験
- 体内実験
化学情報
Publications (30)
溶剤 & 溶解度
- 体外
- 体内
純度とドキュメンテーション
参考文献
Help & FAQs
関連分類
Bioz

生物活性

製品説明

ARV-771 is a BET PROTAC degrader, with K_d values of 34, 4.7, 8.3, 7.6, 9.6 and 7.6 nM against BRD2 (1), BRD2 (2), BRD3 (1), BRD3 (2), BRD4 (1) and BRD4 (2) , respectively. ARV-771 inhibits the transcription of AR/AR-v7 and its downstream target genes. By degrading BRD4 protein, ARV-771 enhances the sensitivity of prostate cancer cells to ferroptosis, suppresses cancer cell viability, and induces apoptosis. ARV-771 downregulates the levels of BRD4, c-MYC and AR-V7 in tumor tissues and inhibits tumor tissue growth. ARV-771 can be used in prostate cancer-related research^[1]^[2]. (Pink: BET ligand (HY-78695); Blue: VHL ligand (HY-112078); Black: linker).

IC₅₀ & Target

^[1]^[2]

BRD2(1)

34 nM (Kd)

BRD2(2)

4.7 nM (Kd)

BRD3(1)

8.3 nM (Kd)

BRD3(2)

7.6 nM (Kd)

BRD4(1)

9.6 nM (Kd)

BRD4(2)

7.6 nM (Kd)

AR-V7

PROTACs アイソフォーム固有の製品をすべて表示 :

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示 :

MCE検証データ

The above results were obtained using AlphaLISA™ SureFire® Ultra™ assays.
The above results were obtained using AlphaLISA™ SureFire® Ultra™ assays.
The above results were obtained using AlphaLISA™ SureFire® Ultra™ assays.

Cellular Effect

Cell Line	Type	Value	Description	References
22Rv1	IC50	10.68 nM	Cytotoxicity against castration-resistant prostate cancer 22Rv1 cells assessed as reduction in cell viability incubated for 72 h by cell viability cytotoxicity assay. Cytotoxicity against castration-resistant prostate cancer 22Rv1 cells assessed as reduction in cell viability incubated for 72 h by cell viability cytotoxicity assay.	41870961
PC-3	IC50	25.19 nM	Cytotoxicity against AR-independent prostate cancer PC-3 cells assessed as reduction in cell viability incubated for 72 h by cell viability cytotoxicity assay. Cytotoxicity against AR-independent prostate cancer PC-3 cells assessed as reduction in cell viability incubated for 72 h by cell viability cytotoxicity assay.	41870961

体外実験

ARV-771 (72 h) potently inhibits cell viability, with an IC₅₀ of 10.68 nM in 22Rv1 cells and 25.19 nM in PC-3 cells; it also induces concentration-dependent BRD4 degradation, with stronger activity observed in 22Rv1 cells^[1].
ARV-771 (3-300 nM; 18 h) induces concentration-dependent degradation of BRD4 in 22Rv1 and PC-3 cells, with stronger activity observed in 22Rv1 cells^[1].
ARV-771 downregulates the expression of BRD4 protein in 22Rv1 cells, and its proteomic profile shows that compared with the ARV@MIL-HA-ss-HA formulation, there are fewer tumor suppressor proteins and more oncoproteins^[1].
ARV-771 (10 nM; 16 h) downregulates FL-AR and AR-V7 mRNA levels in VCaP cells and exerts antiandrogenic effects on multiple AR-regulated genes^[2].
ARV-771 induces apoptosis in 22Rv1 cells, with a total apoptosis rate of 33.25%^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis^[1]

Cell Line:

CRPC 22Rv1 cells, AR-independent prostate cancer PC-3 cells
Concentration:

3, 10, 30, 100 and 300 nM
Incubation Time:

18 h
Result:

Induced concentration-dependent BRD4 protein degradation in both cell lines.
Decreased BRD4 protein levels progressively with increasing ARV-771 concentration, with a more pronounced reduction observed in 22Rv1 cells relative to PC-3 cells at equivalent concentrations.

RT-PCR^[2]

Cell Line:

VCaP cells
Concentration:

10 nM
Incubation Time:

16 h
Result:

Significantly downregulated the mRNA levels of FL-AR and AR-V7.
Exhibited anti-androgenic effects on multiple AR-regulated genes, inhibiting the expression of androgen-responsive genes. Pretreatment for 1 hour completely blocked the expression of the ERG gene induced by the synthetic androgen R1881.
In RNA sequencing experiments in 22Rv1 cells, the expression of seven AR-regulated genes-ELL2, PMEPA1, STEAP1, FAM105A, ATAD2, ENDOD1, and ZNF189-was downregulated by more than 50%.

体内実験

ARV-771 (10 mg/kg; subcutaneous injection; once daily; for 3 consecutive days) downregulates BRD4 and c-MYC levels, respectively, and significantly downregulates AR-V7 levels in tumor tissues of intact male Nu/Nu mice bearing AR-V7+ 22Rv1 tumor xenografts^[2].
ARV-771 (10-30 mg/kg; subcutaneous injection; once daily; for 14 consecutive days) downregulates the levels of both BRD4 and c-MYC in tumor tissues of 22Rv1 tumor xenograft mice, and inhibits tumor growth in these mice in a dose-dependent manner^[2].
ARV-771 (administered subcutaneously; once every 3 days or on a 3-day-on/4-day-off schedule; for a total of 16 days) achieves a 60% tumor growth inhibition rate in VCaP tumor xenograft mice, reduces BRD4 expression by 57% and c-MYC expression by 88% in tumor tissues, and decreases serum PSA by 60%-80%^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male intact Nu/Nu athymic nude mice were used to establish subcutaneous xenograft models using 22Rv1 cells^[2]
Dosage:

10 mg/kg; 20 mg/kg; 30 mg/kg
Administration:

s.c. injection; once daily for 3 days; once daily for 14 days
Result:

It downregulated the levels of BRD4 and c-MYC in mouse tumor tissue by 37% and 76%, respectively, and significantly downregulated AR-V7 levels.
It downregulated the levels of BRD4 and c-MYC in mouse tumor tissue by more than 80%.
Dose-dependent inhibition of tumor growth in mice with 22Rv1 tumor xenografts, with a dose of 30 mg/kg inducing tumor regression; tumors completely disappeared in 2 out of 10 mice.

化学情報

CAS 番号 1949837-12-0
性状 Solid
分子量 986.64
分子式 C₄₉H₆₀ClN₉O₇S₂
Color White to light yellow
SMILES

CC1=C(C)SC2=C1C(C3=CC=C(C=C3)Cl)=N[C@H](C4=NN=C(N42)C)CC(NCCOCCCOCC(N[C@H](C(N5C[C@@H](C[C@H]5C(N[C@@H](C)C6=CC=C(C=C6)C7=C(C)N=CS7)=O)O)=O)C(C)(C)C)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (30)

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Journal Impact Factor

Cell

A TCF4-dependent gene regulatory network confers resistance to immunotherapy in melanoma. [Abstract]

2024 Jan 4;187(1):166-183.e25. PMID: 38181739
Nat Commun

Intrinsic signaling pathways modulate targeted protein degradation. [Abstract]

2024 Jul 2;15(1):5379. PMID: 38956052
J Adv Res

Redistribution of super-enhancers promotes malignancy in human hepatocellular carcinoma. [Abstract]

2025 Jul 4:S2090-1232(25)00504-1. PMID: 40617410
Mol Cell

Cullin-RING ligases employ geometrically optimized catalytic partners for substrate targeting. [Abstract]

2024 Apr 4;84(7):1304-1320.e16. PMID: 38382526

ARV-771 purchased from MedChemExpress. Usage Cited in: Mol Cell. 2024 Apr 4;84(7):1304-1320.e16. [Abstract]

ARV-771 (500 nM; 6 h). Representative western blots comparing protein levels upon treatment with PROTACs in control or UBE2R1/UBE2R2 DKO HEK293T cells. Notice that ectopic expression of either UBE2R1 (lanes 9-12) or UBE2R2 (lanes 13-16) completely restored BRD4 degradation with ARV-771.
Mol Cell

TRIP12 promotes small-molecule-induced degradation through K29/K48-branched ubiquitin chains. [Abstract]

2021 Apr 1;81(7):1411-1424.e7. PMID: 33567268
Mol Cell

Plasticity of the Cullin-RING Ligase Repertoire Shapes Sensitivity to Ligand-Induced Protein Degradation. [Abstract]

2019 Aug 22;75(4):849-858.e8. PMID: 31442425
Nat Chem Biol

Functional E3 ligase hotspots and resistance mechanisms to small-molecule degraders. [Abstract]

2023 Mar;19(3):323-333. PMID: 36329119

ARV-771 purchased from MedChemExpress. Usage Cited in: Nat Chem Biol. 2023 Mar;19(3):323-333. [Abstract]

Heatmap depicting mean log2 fold-enrichment of VHL mutations normalized to maximum log2 fold-changes vs. DMSO across ARV-771 (500 nM; 7 days) treated for 7 days. n = 2 independent measurements.
Nat Chem Biol

Trivalent PROTACs enhance protein degradation via combined avidity and cooperativity. [Abstract]

2021 Nov;17(11):1157-1167. PMID: 34675414
Nat Chem Biol

Rational discovery of molecular glue degraders via scalable chemical profiling. [Abstract]

2020 Nov;16(11):1199-1207. PMID: 32747809
J Control Release

Enhanced protein degradation by intracellular delivery of pre-fused PROTACs using lipid-like nanoparticles. [Abstract]

2021 Feb 10:330:1244-1249. PMID: 33234362
Clin Cancer Res

Overcoming BET Inhibitor Resistance in Malignant Peripheral Nerve Sheath Tumors. [Abstract]

2019 Jun 1;25(11):3404-3416. PMID: 30796033
Nat Struct Mol Biol

CAND1 inhibits Cullin-2-RING ubiquitin ligases for enhanced substrate specificity. [Abstract]

2024 Feb;31(2):323-335. PMID: 38177676
Cell Rep

Functional Genomics Identify Distinct and Overlapping Genes Mediating Resistance to Different Classes of Heterobifunctional Degraders of Oncoproteins. [Abstract]

2021 Jan 5;34(1):108532. PMID: 33406420
J Med Chem

Novel Pyrrolopyridone Bromodomain and Extra-Terminal Motif (BET) Inhibitors Effective in Endocrine-Resistant ER+ Breast Cancer with Acquired Resistance to Fulvestrant and Palbociclib. [Abstract]

2020 Jul 9;63(13):7186-7210. PMID: 32453591
JCI Insight

Epigenetic drug screening defines a PRMT5 inhibitor-sensitive pancreatic cancer subtype. [Abstract]

2022 May 23;7(10):e151353. PMID: 35439169
Biochem Pharmacol

Discovery of a potent BRD4 PROTAC and evaluation of its bioactivity in breast cancer cell lines. [Abstract]

2025 Nov:241:117159. PMID: 40659131
Philos Trans R Soc Lond B Biol Sci

Development of compounds for targeted degradation of mammalian cryptochrome proteins. [Abstract]

2025 Jan 23;380(1918):20230342. PMID: 39842482
Bioorg Chem

A novel Cereblon E3 ligase modulator with antitumor activity in gastrointestinal cancer. [Abstract]

2022 Feb:119:105505. PMID: 34838332
Cancer Sci

MYC Addiction as a Targetable Vulnerability in Nelarabine-Resistant T-Cell Acute Lymphoblastic Leukemia. [Abstract]

2026 Jun;117(6):1608-1622. PMID: 41947770
Structure

PROTAC-mediated activation, rather than degradation, of a nuclear receptor reveals complex ligand-receptor interaction network. [Abstract]

2024 Dec 5;32(12):2352-2363.e8. PMID: 39389062
Curr Issues Mol Biol

Role of the Super-Enhancer Component Bromodomain Protein 4 in the Radiation Response of Human Head and Neck Squamous Cell Carcinoma Cells. [Abstract]

2026 Jan 10;48(1):71. PMID: 41614901
Drug Metab Dispos

Applications of contemporary tools to measure plasma protein binding of targeted protein degraders. [Abstract]

2025 May;53(5):100066. PMID: 40286535
ACS Chem Biol

Cellular Resistance Mechanisms to Targeted Protein Degradation Converge Toward Impairment of the Engaged Ubiquitin Transfer Pathway. [Abstract]

2019 Oct 18;14(10):2215-2223. PMID: 31553577
bioRxiv

2025 April 16.
bioRxiv

2023 Apr 21.
Patent

US20230124700A1.
Patent

US20220288051A1.
Methods Mol Biol

Kinetic Detection of E3:PROTAC:Target Ternary Complexes Using NanoBRET Technology in Live Cells. [Abstract]

2021:2365:151-171. PMID: 34432243
Research Square Preprint

2020 Dec.
Martin-Luther-Universität Halle-Wittenberg

2020 Dec.

溶剤 & 溶解度

体外:

DMSO : ≥ 50 mg/mL (50.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.0135 mL

5.0677 mL

10.1354 mL

5 mM

0.2027 mL

1.0135 mL

2.0271 mL

10 mM

0.1014 mL

0.5068 mL

1.0135 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

モル濃度計算機

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

濃度濃度

体積体積

分子量分子量

希釈計算機

濃度 _(開始) × 体積 _(開始) = 濃度 _(終了) × 体積 _(終了)

濃度 _(開始) 濃度 _(開始)

体積 _(開始) 体積 _(開始)

濃度 _(終了) 濃度 _(終了)

体積 _(終了) 体積 _(終了)

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (2.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (293 KB)
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COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
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MS (2659 KB)
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GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
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取扱説明書 (2659 KB)

参考文献

[1]. Wang C, et al. Nanozyme-Mediated PROTACs Delivery for Targeted Protein Degradation and Ferroptosis Sensitization in Prostate Cancer. Angewandte Chemie (International ed. in English). 2026 May 04;65(19):e6657773.

[2]. Raina K, et al. PROTAC-induced BET protein degradation as a therapy for castration-resistant prostate cancer. Proc Natl Acad Sci U S A. 2016 Jun 28;113(26):7124-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.0135 mL	5.0677 mL	10.1354 mL	25.3385 mL
	5 mM	0.2027 mL	1.0135 mL	2.0271 mL	5.0677 mL
	10 mM	0.1014 mL	0.5068 mL	1.0135 mL	2.5339 mL
	15 mM	0.0676 mL	0.3378 mL	0.6757 mL	1.6892 mL
	20 mM	0.0507 mL	0.2534 mL	0.5068 mL	1.2669 mL
	25 mM	0.0405 mL	0.2027 mL	0.4054 mL	1.0135 mL
	30 mM	0.0338 mL	0.1689 mL	0.3378 mL	0.8446 mL
	40 mM	0.0253 mL	0.1267 mL	0.2534 mL	0.6335 mL
	50 mM	0.0203 mL	0.1014 mL	0.2027 mL	0.5068 mL

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ARV-771

30 Cited Publications

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ARV-771

MedChemExpress（MCE）の使用を引用している文献 ARV-771

PROTACs アイソフォーム固有の製品をすべて表示

Epigenetic Reader Domain アイソフォーム固有の製品をすべて表示

生物活性