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CPI-203

Cat. No. M3526
CPI-203 Structure
Synonym:

CPI203

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 104  USD104 In stock
2mg USD 66  USD66 In stock
5mg USD 120  USD120 In stock
10mg USD 196  USD196 In stock
25mg USD 360  USD360 In stock
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Quality Control & Documentation
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 (for reference only)
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
Chemical Information
Molecular Weight 399.9
Formula C19H18ClN5OS
CAS Number 1446144-04-2
Solubility (25°C) DMSO ≥ 40 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Moros A, et al. Leukemia. Synergistic antitumor activity of lenalidomide with the BET bromodomain inhibitor CPI203 in bortezomib-resistant mantle cell lymphoma.

[2] Devaiah BN, et al. Proc Natl Acad Sci U S A. BRD4 is an atypical kinase that phosphorylates serine2 of the RNA polymerase II carboxy-terminal domain.

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Keywords: CPI-203, CPI203 supplier, Epigenetic Reader Domain, inhibitors, activators


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