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CPI-203

Cat. No. M3526
CPI-203 Structure
Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL In DMSO USD 110 In stock
2mg USD 75 In stock
5mg USD 120 In stock
10mg USD 200 In stock
25mg USD 360 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

CPI-203 is a potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM. CPI-203 inhibits BRD4 in vitro and in cells, but it 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. CPI-203 arrests the growth of leukemic T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice. In contrast, in vivo, specific Ser2 phosphorylation by either endogenous BRD4 or exogenous BRD4 FEE-AAA was markedly decreased by treatment with the inhibitor.

Customer Product Validations & Biological Datas
Source Genes Dev (2015). Figure 6. CPI-203
Method qRT–PCR
Cell Lines LSK CD150+ CD48− HSCs
Concentrations 0.5 μM
Incubation Time 24 h
Results As expected, MycmRNAwas reduced by twofold to threefold compared with mock-treated HSCs in both groups, while there was no difference in Myc expression between the Erg+/− and Erg+/+ groups
Protocol
Cell Experiment
Cell lines 2 PBMC cultures from healthy donors and 9 MCL cell lines (Granta-519, JVM-2, UPN1, Z-138, JeKo-1, ZBR, JBR, Mino, REC-1 cells)
Preparation method Incubating MCL primary cells and cell lines as indicated with lenalidomide and/or CPI203. Adding MTT for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Using untreated control cells to represent values . The GI50 is calculated as the concentration that produced 50 % growth inhibition. Using the Calcusyn software version 2.0 to calculate Combination indexes (CIs) . When CI <1 ,the interaction between two drugs is considered synergistic.
Concentrations 10 μM
Incubation time 72 hours
Animal Experiment
Animal models REC-1 tumor-bearing mice
Formulation
Dosages 2.5 mg/kg twice daily
Administration i.p
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 399.9
Formula C19H18ClN5OS
CAS Number 1446144-04-2
Purity >98%
Solubility DMSO
Storage at -20°C
References

Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma.
Moros A, et al. Leukemia. 2014 Mar 18. PMID: 24721791.

BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain.
Devaiah BN, et al. Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32. PMID: 22509028.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: CPI-203 supplier, Epigenetic Reader Domain, inhibitors

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