CPI-203(RO-6870810,TEN-010,JQ2,and RG-6146)

Molecular Weight (MW)	399.90
Formula	C19H18ClN5OS
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
Synonyms	RO-6870810; CPI203; CPI-203; CPI 203;RO 6870810; TEN010; RG 6146; RG-6146; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RO6870810;

Molecular Weight (MW)

399.90

Formula

C19H18ClN5OS

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

Synonyms

RO-6870810; CPI203; CPI-203; CPI 203;RO 6870810; TEN010; RG 6146; RG-6146; TEN 010; TEN010; JQ-2; JQ 2; JQ2; RG-6146; RO6870810;

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 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
Animal model	Treatment 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 & Dosage	2.5 mg/kg i.p.
References	Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.

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 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

Animal model

Treatment 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 & Dosage

2.5 mg/kg i.p.

References

Proc Natl Acad Sci U S A. 2012 May 1;109(18):6927-32.

CAS NO:	1446144-04-2
规格:	≥98%

包装	价格(元)
5mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议