2. Epigenetics
  3. Epigenetic Reader Domain
  4. RVX-297

RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models.

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RVX-297 Chemical Structure

RVX-297 Chemical Structure

CAS No. : 1044871-04-6

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Based on 1 publication(s) in Google Scholar

RVX-297 Related Antibodies

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Description

RVX-297 is a potent, orally active BET bromodomain inhibitor with selectivity for BD2. RVX-297 shows IC50s of 0.08, 0.05, and 0.02 μM for BRD2(BD2), BRD3(BD2), and BRD4(BD2), respectively. RVX-297 suppresses inflammatory gene expression in multiple immune cell types. RVX-297 is effective in acute inflammation and autoimmunity models[1][2].

IC50 & Target[2]

BRD2 (BD1)

3.76 μM (IC50)

BRD2 (BD2)

0.08 μM (IC50)

BRD3 (BD1)

2.34 μM (IC50)

BRD3 (BD2)

0.05 μM (IC50)

BRD4 (BD1)

1.16 μM (IC50)

BRD4 (BD2)

0.02 μM (IC50)

BRDT (BD1)

2.69 μM (IC50)

In Vitro

RVX-297 (1-30 μM; 24 hours) decreases proinflammatory gene expression in synovial fibroblasts[1].
RVX-297 displaces BET proteins from the promoters of sensitive genes and disrupted recruitment of active RNA polymerase II, a property shared with pan-BET inhibitors that nonselectively bind BET BDs[1].
RVX-297 reduces gene expression of inflammatory mediators in vitro. RVX-297 suppresses IL-6 gene induction in human U937 macrophages, mouse primary B cells isolated from the spleen, mouse BMDMs, and THP-1 monocytes in a dose-dependent manner. RVX-297 represses IL-1β expression in LPS-stimulated mouse BMDMs, with an IC50 of 0.4-3 μM. RVX-297 inhibits MCP-1 expression in unstimulated human PBMCs with an IC50 of 0.4 μM. RVX-297 inhibits antigen stimulation of T cells and the induction of IL-17 expression[1].

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

RVX-297 Related Antibodies

RT-PCR[1]

Cell Line: Synovial fibroblasts
Concentration: 1-30 μM
Incubation Time: 24 hours
Result: Downregulated IL-6 and VCAM-1 gene expression in synovial fibroblasts.
In Vivo

RVX-297 (25-75 mg/kg; p.o.; per day for 6 day) inhibits progression of pathology in the rat collagen-induced arthritis model[1].
RVX-297 (75-150 mg/kg) inhibits progression of pathology in the mouse collagen-induced arthritis model[1].
RVX-297 suppresses cytokine production in LPS-treated mice[1].

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

Animal Model: Female Lewis rats are 6-8 weeks old, approximately 150 g (rat collagen-induced arthritis)[1]
Dosage: 25, 50, and 75 mg/kg
Administration: P.o.; per day for 6 days
Result: Prevented swelling and inflammation of the ankle and knee joints.
Molecular Weight

423.50

Formula

C24H29N3O4
CAS No.
Appearance

Solid

Color

White to light brown

SMILES

O=C1NC(C2=CC(C)=C(OCCN3CCCC3)C(C)=C2)=NC4=C1C(OC)=CC(OC)=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (118.06 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3613 mL 11.8064 mL 23.6128 mL
5 mM 0.4723 mL 2.3613 mL 4.7225 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

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: ≥ 2.08 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.91 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.3613 mL 11.8064 mL 23.6128 mL 59.0319 mL
5 mM 0.4723 mL 2.3613 mL 4.7226 mL 11.8064 mL
10 mM 0.2361 mL 1.1806 mL 2.3613 mL 5.9032 mL
15 mM 0.1574 mL 0.7871 mL 1.5742 mL 3.9355 mL
20 mM 0.1181 mL 0.5903 mL 1.1806 mL 2.9516 mL
25 mM 0.0945 mL 0.4723 mL 0.9445 mL 2.3613 mL
30 mM 0.0787 mL 0.3935 mL 0.7871 mL 1.9677 mL
40 mM 0.0590 mL 0.2952 mL 0.5903 mL 1.4758 mL
50 mM 0.0472 mL 0.2361 mL 0.4723 mL 1.1806 mL
60 mM 0.0394 mL 0.1968 mL 0.3935 mL 0.9839 mL
80 mM 0.0295 mL 0.1476 mL 0.2952 mL 0.7379 mL
100 mM 0.0236 mL 0.1181 mL 0.2361 mL 0.5903 mL
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RVX-297 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:

RVX-2971044871-04-6RVX297RVX 297Epigenetic Reader DomainselectivityinflammatoryimmunecellacuteautoimmunitymediatorproinflammatoryarthritisInhibitorinhibitorinhibit

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