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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 |
---|---|---|---|
1 mg | 39 € | In Stock | |
5 mg | 93 € | In Stock | |
10 mg | 154 € | In Stock | |
25 mg | 311 € | In Stock | |
50 mg | 502 € | In Stock | |
100 mg | 810 € | In Stock | |
1 mL x 10 mM (in DMSO) | 102 € | 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 | BRDT BD1:2.69 μM, BRD3 BD1:2.34 μM, BRD3 BD2:0.05 μM, BRD4 BD1:1.16 μM, BRD2 BD1:3.76 μM, BRD4 BD2:0.02 μM, BRD2 BD2:0.08 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]. |
Alias | 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) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||
Solubility Information | DMSO: 40 mg/mL (94.45 mM) | ||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||
DMSO
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