CPI203, BET bromodomain inhibitor (TBI4048)

Description

Product Details

Formal Name: (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

Alternate Names: CPI-267203; 2-[(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

Molecular Formula: C₁₉H₁₈ClN₅OS

Formula Weight: 399.90

CAS Number: 1446144-04-2

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to at least 25 mg/ml)

Storage: -20°C

Stability: ≥ 1 year.

Applications

BET bromodomain inhibitor

Functions

CPI203, a JQ1 analog, is a potent and selective inhibitor of the BET bromodomain BRD4 (IC50 = 26 nM). It helps promote the maintenance of hematopoietic stem cells via repression of Myc expression. CPI203 reversibly suppressed intestinal stem cell differentiation in a mouse model. It enhanced the expansion of human cord blood hematopoietic stem cells without losing cell viability. CPI203 displays synergistic antitumor activity with various agents including lenalidomide, bortezomib, and PARP inhibitors.

Application Procedures

First dissolved in DMSO (up to at least 25 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20° for up to 3 months.