| Identification | Back Directory | [Name]
Benzenesulfonamide, N-[2,3-dihydro-3-(1-methylethylidene)-2-oxo-1H-indol-5-yl]-2-methoxy- | [CAS]
2490311-14-1 | [Synonyms]
CUN11141
BRD4 Inhibitor-20
Benzenesulfonamide, N-[2,3-dihydro-3-(1-methylethylidene)-2-oxo-1H-indol-5-yl]-2-methoxy- | [Molecular Formula]
C18H18N2O4S | [MOL File]
2490311-14-1.mol | [Molecular Weight]
358.41 |
| Hazard Information | Back Directory | [Uses]
BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer[1]. | [in vivo]
BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie[1]. | Animal Model: | rats[1] | | Dosage: | 5 mg/kg, 15 mg/kg | | Administration: | intravenous dosing (iv) or oral dosing (po) | | Result: | | PK Parameters | iv (5 mg/kg) | po (15 mg/kg) | | Cmax(μg/L) | - | 2175 | | Tmax(h) | - | 1.00 | | t1/2(h) | 1.56 | 3.59 | | CLz/F (L/h/kg) | 0.68 | 1.03 | | AUC0?t(μg/L*h) | 7296 | 14384 | | AUC0?∞(μg/L*h) | 7340 | 14600 | | F (%) | - | 66% | |
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| [IC 50]
BRD4 BD1: 19 nM (IC50); BRD4 BD2: 28 nM (IC50); BRD2 (BD1): 24 nM (IC50); BRD2 (BD2): 18 nM (IC50) | [References]
[1] Yu Xu, et al. Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. Eur J Med Chem. 2020 Dec 15;208:112780. DOI:10.1016/j.ejmech.2020.112780 |
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