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dBET6

SKU: orb1302063

Description

dBET6

Research Area

Cell Biology, Epigenetics & Chromatin, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number1950634-92-0
MW841.37
Purity97.57% (May vary between batches)
FormulaC42H45ClN8O7S
SMILESCC=1C2=C(N3C([C@H](CC(NCCCCCCCCNC(COC4=C5C(C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=CC=C4)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C
TargetApoptosis,Epigenetic Reader Domain,PROTACs
Solubility10% DMSO+90% Corn Oil:1 mg/mL (1.19 mM);DMSO:112.5 mg/mL (133.71 mM)

Bioactivity

Target IC50
BET:14 nM
In Vivo
dBET6 (7.5 mg/kg, p.o., BID) reduces leukemic burden in a disseminated mouse model of T-ALL.
In Vitro
dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4.
Animal Research
MOLT4 human T-ALL cells are intravenously injected into NSG mice (2×106 cells/mouse). Luminescence is utilized to monitor engraftment (evident at day 6), at which point mice are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 8), JQ1 (20 mg/kg QD, n = 9) or vehicle (captisol, n = 9) treatment for 14 days. Survival of all three cohorts is subsequently monitored using hind limb paralysis caused by a high femoral leukemic burden as a defined endpoint. SUPT11 human T-ALL cells (mCherry+ and Luciferase+) are intravenously injected into NSG mice (2.52×106 cells/mouse). Luminescence is used to monitor successful engraftment, occurring 10 days after injection. At this point, animals are randomized into three cohorts that receive dBET6 (7.5 mg/kg BID, n = 7), JQ1 (7.5 mg/kg BID, n = 7) or vehicle (captisol, n = 7) treatment for 18 days. Treatment burden is assessed via total body luminescence imaging as well as by bone marrow infiltration by mCherry+ T-ALL cells.

Storage & Handling

Storage-20°C
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

dBET 6, dBET6, dBET-6, BET, Apoptosis, Epigenetic Reader Domain, EpigeneticReaderDomain, Inhibitor, inhibit, PROTACs

Similar Products

  • dBET6 [orb1225790]

    >98% (HPLC)

    1950634-92-0

    841.381

    C42H45ClN8O7S

    1 g, 50 mg, 100 mg, 500 mg, 5 mg, 10 mg, 25 mg
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Key Properties

No computed properties available.

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Protocol Information

dBET6 (orb1302063)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 1,170.00
5 mg
¥ 1,820.00
1 ml x 10 mM (in DMSO)
¥ 2,600.00
10 mg
¥ 2,860.00
25 mg
¥ 4,810.00
50 mg
¥ 7,280.00
100 mg
¥ 10,270.00
200 mg
¥ 12,870.00
500 mg
¥ 18,460.00
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