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1883863-52-2

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1883863-52-2 Structure

1883863-52-2 Structure
IdentificationBack 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 PropertiesBack 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
Safety DataBack Directory
[Symbol(GHS) ]

Exclamation Mark (GHS07)
GHS07
[Signal word ]

Warning
[Hazard statements ]

H302-H315-H319-H335
[Precautionary statements ]

P261-P305+P351+P338
Hazard InformationBack 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
Spectrum DetailBack Directory
[Spectrum Detail]

dBET57(1883863-52-2)1HNMR
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