ARV-771

Name: ARV-771
Brand: MedChemExpress
SKU: HY-100972
Rating: 5.0 (29 reviews)

Cat. No.: HY-100972 Purity: 99.82%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

ARV-771 is a potent BET PROTAC based on E3 ligase von Hippel-Lindau with K_ds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.

For research use only. We do not sell to patients.

CAS No. : 1949837-12-0

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

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Customer Review

Based on 29 publication(s) in Google Scholar

Other Forms of ARV-771:

ARV-771 (Standard) Get quote

29 Publications Citing Use of MCE ARV-771

Others

: 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.

: 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.

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von Hippel-Lindau (VHL) Cereblon MDM2 cIAP1

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

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)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.64 μM Compound: ARV-771	Antiproliferative activity against human normal (non-senescent) A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human normal (non-senescent) A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38635879]
A549	IC₅₀	603 nM Compound: ARV-771	Antiproliferative activity against human senescent A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human senescent A549 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38635879]
CWR22R	EC₅₀	44 nM Compound: 22; ARV-771	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-Glo cell viability assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 72 hrs by Celltiter-Glo cell viability assay	[PMID: 34881891]
EOL1	IC₅₀	1.5 nM Compound: ARV-771; 34	Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth Antiproliferative activity against human EOL1 cells assessed as inhibition of cell growth	[PMID: 36202064]
HFF-1	IC₅₀	1.1 μM Compound: ARV-771	Antiproliferative activity against human HFF-1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HFF-1 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38160619]
HK-2	IC₅₀	0.16 μM Compound: ARV-771	Antiproliferative activity against human HK-2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HK-2 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38160619]
HL-60	IC₅₀	1.5 nM Compound: ARV-771; 34	Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth	[PMID: 36202064]
HeLa	IC₅₀	183 nM Compound: 35; ARV-771	Antiproliferative activity against human HeLa cells Antiproliferative activity against human HeLa cells	[PMID: 35763424]
HeLa	IC₅₀	183 nM Compound: ARV-771	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38160619]
MCF7	IC₅₀	120.4 nM Compound: ARV-771	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo luminescent assay	[PMID: 38160619]
MOLM-13	IC₅₀	7.45 nM Compound: ARV-771	Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay Growth inhibition of human MOLM13 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
MV4-11	IC₅₀	0.43 nM Compound: ARV-771	Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay Growth inhibition of human MV4-11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
NIH3T3	IC₅₀	0.21 μM Compound: ARV-771	Antiproliferative activity against mouse 3T3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against mouse 3T3 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38160619]
OVCAR-8	IC₅₀	215 nM Compound: ARV-771	Antiproliferative activity against human OVCAR-8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human OVCAR-8 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38160619]
RS4-11	IC₅₀	2.4 nM Compound: ARV-771	Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay Growth inhibition of human RS4:11 cells after 96 hrs by CCK8 assay	[PMID: 30019901]
T47D	IC₅₀	13 nM Compound: ARV-771	Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human T47D cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay	[PMID: 38160619]
VCaP	DC₅₀	< 5 nM Compound: 101; ARV-771	Degradation of BRD4 in human VCaP cells after 16 hrs by Western blot analysis Degradation of BRD4 in human VCaP cells after 16 hrs by Western blot analysis	[PMID: 30542529]
VCaP	DC₅₀	< 5 nM Compound: 47; ARV-771	Protac activity against VHL/BRD3 in human VCaP cells assessed as induction of BRD3 protein degradation by reverse phase protein array analysis Protac activity against VHL/BRD3 in human VCaP cells assessed as induction of BRD3 protein degradation by reverse phase protein array analysis	[PMID: 31035238]
Z-138	IC₅₀	142 nM Compound: 101; ARV-771	Induction of apoptosis in human ibrutinib-resistant Z138 cells after 48 hrs by Annexin-V/propidium iodide staining based assay Induction of apoptosis in human ibrutinib-resistant Z138 cells after 48 hrs by Annexin-V/propidium iodide staining based assay	[PMID: 30542529]

In Vitro

ARV-771, a small-molecule pan-BET PROTAC degrader, 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].

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

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].

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

Molecular Weight

986.64

Formula

C₄₉H₆₀ClN₉O₇S₂

CAS No.

1949837-12-0

Appearance

Solid

Color

White to light yellow

SMILES

CC(C(C(C1=CC=C(Cl)C=C1)=N[C@@H](CC(NCCOCCCOCC(N[C@@H](C(C)(C)C)C(N(C[C@H](O)C2)[C@@H]2C(N[C@H](C3=CC=C(C(SC=N4)=C4C)C=C3)C)=O)=O)=O)=O)C5=NN=C(C)N65)=C6S7)=C7C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (273 KB) SDS (394 KB)

COA (245 KB) HNMR (322 KB) RP-HPLC (245 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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. 2016 Jun 28;113(26):7124-9. [Content Brief]

Cell Assay ^[1]	ARV-771 is dissolved in DMSO. 22Rv1 cells (5,000 cells per well) are dosed with ARV-771 serially diluted 1:3 for a 10-point dose curve for 72 h. CellTiter-Glo Luminescent Cell Viability Assay is added, and the plate is read on a luminometer. Data are analyzed and plotted using GraphPad Prism software^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[1]	Mice: Mice bearing tumors are treated with ARV-771 (5, 10, 30, 50 mg/kg) for up to 3 wk, depending on the experiment. Mice are sacrificed 8 h after the final dose. Plasma and tissues are harvested and flash frozen for further analysis^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[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. 2016 Jun 28;113(26):7124-9. [Content Brief]

Complete Stock Solution Preparation Table

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

ARV-771 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ARV-7711949837-12-0ARV771ARV 771PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

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ARV-771

Customer Review

Other Forms of ARV-771:

ARV-771 Related Antibodies

29 Publications Citing Use of MCE ARV-771

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Biological Activity

Protocol

Purity & Documentation

References

Customer Review

ARV-771 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

ARV-771 Related Classifications

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