[CAS NO. 1446144-04-2] CPI-203
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PRODUCTS SPECIFICATIONS [1446144-04-2]
Store
Catalog
SLK-S7304
Brand
Selleck
CAS
1446144-04-2
DESCRIPTION [1446144-04-2]
Overview
| MDL | MFCD27997886 |
|---|---|
| Molecular Weight | 399.90 |
| Molecular Formula | C19H18ClN5OS |
| SMILES | O=C(N)C[C@H]1C2=NN=C(C)N2C3=C(C(C)=C(C)S3)C(C4=CC=C(Cl)C=C4)=N1 |
For research use only.
Storage
3 years,-20°C,powder
1 years,-80°C,in solvent
1 years,-80°C,in solvent
Shipping
Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)
Preparing Stock Solutions
| 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5006 mL | 12.5031 mL | 25.0063 mL |
| 5 mM | 0.5001 mL | 2.5006 mL | 5.0013 mL |
| 10 mM | 0.2501 mL | 1.2503 mL | 2.5006 mL |
| 50 mM | 0.0500 mL | 0.2501 mL | 0.5001 mL |
Description
CPI-203 is a potent inhibitor with of 37 nM for BRD4.
In vitro
CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. 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.
In vivo
BRD4 mediates CTD Ser2 phosphorylation in vivo. In REC-1 tumor-bearing mice, the combination of lenalidomide with CPI203 (2.5 mg/kg i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis.
References
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