keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 48.00 | |
5 mg | In stock | $ 98.00 | |
10 mg | In stock | $ 172.00 | |
25 mg | In stock | $ 323.00 | |
50 mg | In stock | $ 518.00 | |
100 mg | In stock | $ 749.00 | |
200 mg | In stock | $ 945.00 | |
500 mg | In stock | $ 1,380.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 159.00 |
Description | dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity. |
Targets&IC50 | BET:14 nM |
In vitro | dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4. |
In vivo | dBET6 (7.5 mg/kg, p.o., BID) decreases the leukemic burden in a disseminated mouse model of T-ALL. |
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. |
Molecular Weight | 841.37 |
Formula | C42H45ClN8O7S |
CAS No. | 1950634-92-0 |
keep away from direct sunlight
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 10 mM
You can also refer to dose conversion for different animals. More
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dBET6 1950634-92-0 Apoptosis Chromatin/Epigenetic Epigenetic Reader Domain dBET-6 PROTACs Inhibitor inhibit dBET 6 inhibitor