dBET6, CAS 1950634-92-0

Formulation: A solid

Formal Name: (6S)-4-(4-chlorophenyl)-N-[8-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]octyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

Purity: ≥98%

Formula Markup: C42H45ClN8O7S

Formula Weight: 841,4

Shelf life (days): 1460

CAS Number: 1950634-92-0

Notes: dBET6 is a hybrid compound that drives the selective proteasomal degradation of bromodomain-containing protein 4 (BRD4).{63349} It is characterized as a proteolysis-targeting chimera (PROTAC) and contains JQ1, which binds bromo- and extra-terminal (BET) proteins, linked to thalidomide, a ligand for the E3 ubiquitin ligase cereblon.{63350} dBET6 binds to BRD4 (IC50 = 14 nM) and induces its degradation when used at a concentration of 100 nM, leading to a global inhibition of transcription in MOLT-4 T cell acute lymphoblastic leukemia (T-ALL) cells.{63349} It also reduces leukemic burden in a MOLT-4 T-ALL mouse xenograft model when administered at a dose of 7.5 mg/kg twice per day.

• Artikelnummer: CAY35385-50
• Hersteller: Cayman Chemical
• Hersteller Artikelnummer: 35385-50
• Green Labware: Nein
• Verpackungseinheit: 50 mg
• Mengeneinheit: STK