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RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 5 mg | $41 | In Stock | |
| 10 mg | $68 | In Stock | |
| 25 mg | $138 | In Stock | |
| 50 mg | $222 | In Stock | |
| 100 mg | $358 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $46 | In Stock |
| Description | RVX-297 is a BD2 selective inhibitor of BET bromodomains. RVX-297 preferentially binds to the BD2 domains of the BET bromodomain and Extra Terminal (BET) family of protein. |
| Targets&IC50 | BRD4 BD2:0.02 μM, BRD3 BD2:0.05 μM, BRD3 BD1:2.34 μM, BRDT BD1:2.69 μM, BRD2 BD2:0.08 μM, BRD4 BD1:1.16 μM, BRD2 BD1:3.76 μM |
| In vitro | RVX-297 suppressed 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[2]. |
| In vivo | In the rCIA model, RVX-297 treatment had a substantial impact on cytokine gene expression; expressions of IL-1β, RANKL, MMP3, and MMP13 were all significantly decreased in the ankle joints of arthritic rats after RVX-297 treatment at 75 mg/kg BID versus vehicle-treated arthritic controls[2]. |
| Synonyms | RVX297 |
| Molecular Weight | 423.5 |
| Formula | C24H29N3O4 |
| Cas No. | 1044871-04-6 |
| Smiles | COc1cc(OC)c2c(c1)nc([nH]c2=O)-c1cc(C)c(OCCN2CCCC2)c(C)c1 |
| Relative Density. | 1.25 g/cm3 (Predicted) |
| Color | White |
| Appearance | Solid |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | ||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (94.45 mM), Sonication is recommended. | ||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.72 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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