ARV-825

Name: ARV-825
Brand: MedChemExpress
SKU: HY-16954
Rating: 5.0 (23 reviews)

Cat. No.: HY-16954 Purity: 99.32%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

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

ARV-825 Chemical Structure

CAS No. : 1818885-28-7

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 280	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 280	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 180	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 220	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 450	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 750	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 23 publication(s) in Google Scholar

20 Publications Citing Use of MCE ARV-825

: ARV-825 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 14;11(1):4083. [Abstract]; Cells treated with ARV-825 shows marked degradation of BRD4 protein and significantly reduces levels of MYC protein, demonstrating reduced levels of BRD4-driven MYC transcription.

: ARV-825 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2020 Aug 14;11(1):4083. [Abstract]; Representative IF images and quantification of nuclear S9.6 intensity, γH2AX foci, and RNase H1 in HeLa cells in the absence (−DOX) or presence (+DOX) of doxycycline-induced FLAG-tagged RNase H1 expression for 24 h, followed by treatment with 100 nM ARV-825 for 6 h.

: ARV-825 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Sep 5;8(1):13225. [Abstract]; ARV-825 decreases IFN-γ-induced PD-L1 mRNA and protein expression in primary PSCs and in the stellate cell line.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

ARV-825 is a PROTAC connected by ligands for Cereblon and BRD4. ARV-825 binds to BD1 and BD2 of BRD4 with K_ds of 90 and 28 nM, respectively.

IC₅₀ & Target

Kd: 90 nM (Bromodomain 1 of BRD4), 28 nM (Bromodomain 2 of BRD4)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
MOLM-13	IC₅₀	18.2 nM Compound: ARV-825	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]
MOLM-13	IC₅₀	18.2 nM Compound: 6; ARV-825	Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human MOLM13 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]
MV4-11	IC₅₀	1.05 nM Compound: ARV-825	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]
RS4-11	IC₅₀	3.3 nM Compound: ARV-825	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]
RS4-11	IC₅₀	3.3 nM Compound: 6; ARV-825	Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay Cytotoxicity against human RS4:11 cells assessed as cell growth inhibition after 4 days by WST-8 assay	[PMID: 28339196]

In Vitro

ARV-825 is a hetero-bifunctional proteolysis-targeting chimera (PROTAC) that recruits BRD4 to the E3 ubiquitin ligase cereblon. ARV-825 actively recruits BRD4 to cereblon, resulting in the rapid and efficient degradation of the former via the proteasome. Given that BRD4 and cereblon binding moieties in ARV-825 have K_ds of 28-90 nM and ~3 μM to their respective targets, this suggests that ARV-825 acts in a substoichiometric way in mediating BRD4 degradation. ARV-825 treatment results in prolonged BRD4 down-regulation and downstream signaling suppression compared to BRD4 inhibitors^[1].

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

Molecular Weight

923.43

Formula

C₄₆H₄₇ClN₈O₉S

CAS No.

1818885-28-7

Appearance

Solid

Color

Light yellow to yellow

SMILES

CC1=NN=C2N1C(SC(C)=C3C)=C3C(C4=CC=C(Cl)C=C4)=N[C@H]2CC(NC5=CC=C(OCCOCCOCCOCCNC6=C(C(N(C7CCC(NC7=O)=O)C8=O)=O)C8=CC=C6)C=C5)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (54.15 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	1.0829 mL	5.4146 mL	10.8292 mL
5 mM	0.2166 mL	1.0829 mL	2.1658 mL
10 mM	0.1083 mL	0.5415 mL	1.0829 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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 (2.71 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% Corn Oil
Solubility: ≥ 2.5 mg/mL (2.71 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: 99.32%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (248 KB) LCMS (108 KB)

Handling Instructions (2659 KB)

References

[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. [Content Brief]

Kinase Assay ^[1]	Affinity of compounds (e.g., ARV-825) with Bromodomain 1 and 2 of BRD4 is determined with BROMOscan by DiscoverX^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References	[1]. Lu J, et al. Hijacking the E3 Ubiquitin Ligase Cereblon to Efficiently Target BRD4. Chem Biol. 2015 Jun 18;22(6):755-63. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.0829 mL	5.4146 mL	10.8292 mL	27.0730 mL
	5 mM	0.2166 mL	1.0829 mL	2.1658 mL	5.4146 mL
	10 mM	0.1083 mL	0.5415 mL	1.0829 mL	2.7073 mL
	15 mM	0.0722 mL	0.3610 mL	0.7219 mL	1.8049 mL
	20 mM	0.0541 mL	0.2707 mL	0.5415 mL	1.3536 mL
	25 mM	0.0433 mL	0.2166 mL	0.4332 mL	1.0829 mL
	30 mM	0.0361 mL	0.1805 mL	0.3610 mL	0.9024 mL
	40 mM	0.0271 mL	0.1354 mL	0.2707 mL	0.6768 mL
	50 mM	0.0217 mL	0.1083 mL	0.2166 mL	0.5415 mL

ARV-825 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-8251818885-28-7ARV825ARV 825PROTACsEpigenetic Reader DomainInhibitorinhibitorinhibit

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ARV-825

Customer Review

ARV-825 Related Antibodies

20 Publications Citing Use of MCE ARV-825

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•Related Screening Libraries:

•Related Small Molecules:

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View All PROTACs Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

ARV-825 Related Antibodies

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Dilution Calculator

Complete Stock Solution Preparation Table

ARV-825 Related Classifications

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