| Identification | Back Directory | [Name]
dBET57 | [CAS]
1883863-52-2 | [Synonyms]
dBET57
DBET57;DBET 57;DBET-57
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethyl]-2,3,9-trimethyl-, (6S)- | [Molecular Formula]
C34H31ClN8O5S | [MOL File]
1883863-52-2.mol | [Molecular Weight]
699.18 |
| Chemical Properties | Back Directory | [density ]
1.60±0.1 g/cm3(Predicted) | [storage temp. ]
4°C, protect from light | [solubility ]
DMSO: soluble | [form ]
A solid | [pka]
10.74±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
dBET57 is a BRD4 selective degrader. | [in vivo]
dBET57 (7.5 mg/kg, intraperitoneal injection, once daily, 2 weeks) has antitumor activity in the SK-NBE(2) xenograft mouse model[1]. | Animal Model: | SK-NBE(2) xenograft mouse model[1] | | Dosage: | 7.5 mg/kg, daily, 2 weeks | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Reduced tumor volume, decreased the proportion of ki-67 positive cells, increased the proportion of caspase3, had no obvious organ toxicity, and downregulated the level of ZMYND8. |
| [IC 50]
BRD4 (BD1): 500 nM (DC50) | [storage]
4°C, protect from light |
|
|