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CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 2 mg | $30 | In Stock | In Stock | |
| 5 mg | $53 | In Stock | In Stock | |
| 10 mg | $86 | In Stock | In Stock | |
| 25 mg | $188 | In Stock | In Stock | |
| 50 mg | $298 | - | In Stock | |
| 100 mg | $472 | - | In Stock | |
| 200 mg | $659 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $56 | In Stock | In Stock |
| Description | CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4). |
| Targets&IC50 | BRD4:37 nM |
| In vitro | CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. [1] CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. [2] |
| Kinase Assay | BRD4 α-screen assay: The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor. |
| Synonyms | CPI203, CPI 203 |
| Molecular Weight | 399.9 |
| Formula | C19H18ClN5OS |
| Cas No. | 1446144-04-2 |
| Smiles | Cc1nnc2[C@H](CC(N)=O)N=C(c3c(C)c(C)sc3-n12)c1ccc(Cl)cc1 |
| Relative Density. | 1.51 g/cm3 (Predicted) |
| 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: 50 mg/mL (125.03 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5 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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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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