DC Chemicals · Product datasheet

CPI203 (CPI-203) — Datasheet

CAT. NO. DC5046

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ParameterValue
Chemical Name2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaen-9-yl]acetamide
CAS No.1446144-04-2
SynonymsCPI 203;CPI-203;6H-​Thieno[3,​2-​f]​[1,​2,​4]​triazolo[4,​3-​a]​[1,​4]​diazepine-​6-​acetamide, 4-​(4-​chlorophenyl)​-​2,​3,​9-​trimethyl-​, (6S)​-;(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide;CPI203;C19H18ClN5OS;(s)-2-(4-(4-chlorophenyl)-2,3,9-trimethyl-6h-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepin-6-yl)acetamide;GTPL7513;AOB6784;s7304;2338AH;SB19335;CPI203, >=98% (HPLC);BC600523;SW219296-1;8-{(1S)-1-[8-(Triflu;2-[(9S)-7-(4-Chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6)
FormulaC19H18ClN5OS
M.Wt399.8971
SMILESClC1C([H])=C([H])C(=C([H])C=1[H])C1C2C(C([H])([H])[H])=C(C([H])([H])[H])SC=2N2C(C([H])([H])[H])=NN=C2[C@]([H])(C([H])([H])C(N([H])[H])=O)N=1
Purity>99%, ee>99%
Storage2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Biological Activity

CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC50 value of appr 37 nM (BRD4 α-screen assay).

In Vitro

CPI203 inhibits BRD4 in vitro and in cells, but does not affect BRD4 kinase activity in vitro[1]. 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[2].

In Vivo

BRD4 mediates CTD Ser2 phosphorylation in vivo[1]. 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[2].

References & source

DC Chemicals original product information

Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.

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