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CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $30 | In Stock | |
5 mg | $53 | In Stock | |
10 mg | $86 | In Stock | |
25 mg | $188 | 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 |
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. |
Alias | 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. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 50 mg/mL (125.03 mM) | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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