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CPI-203(RO-6870810,TEN-010,JQ2,and RG-6146)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
CPI-203(RO-6870810,TEN-010,JQ2,and RG-6146)图片
CAS NO:1446144-04-2
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)399.90
FormulaC19H18ClN5OS
CAS No.1446144-04-2
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 79 mg/mL (197.54mM)
Water: <1 mg/mL
Ethanol: 5 mg/mL (12.5 mM)
Solubility (In vivo)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
SynonymsRO-6870810; CPI203; CPI-203; CPI 203;RO 6870810; TEN010; RG 6146; RG-6146; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RO6870810;
实验参考方法
In Vitro

In vitro activity: 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


Kinase 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.


Cell Assay: MCL primary cells and 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)) are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI<1.

In VivoBRD4 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
Animal modelTreatment with JQ1 derivative CPI203 inhibits BRD4 phosphorylation of CTD Ser2 in vivo. HeLa cells were transfected as above and treated with increasing concentrations of CPI203.
Formulation & Dosage2.5 mg/kg i.p.
References Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.