首页Chromatin/EpigeneticEpigenetic Reader DomaindBET6
dBET6
编号 T5130    
CAS 1950634-92-0     分子式 C42H45ClN8O7S     分子量 841.37
靶点: BET;
dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.
纯度:98.76%
规格 库存 单价 数量
1 mg 上海现货 320.00
5 mg 上海现货 960.00
10 mg 上海现货 1700.00
25 mg 上海现货 3660.00
1 mL * 10 mM (in DMSO) 上海现货 1828.00
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生物活性

产品描述

dBET6 is a selective and cell-permeable degrader of BET based on PROTAC (IC50: 14 nM). It has antitumor activity.

靶点活性

BET,14 nM

体外活性

dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4.

体内活性

dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL.

动物实验

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.

化学信息

分子量

841.37

分子式

C42H45ClN8O7S

CAS

1950634-92-0

溶解度

DMSO: 10 mM

( < 1 mg/ml refers to the product slightly soluble or insoluble )

储存条件

store at -80°C

备注

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

配制溶液

1 mg 5 mg 10 mg
1 mM 1.189 ml 5.943 ml 11.885 ml
5 mM 0.238 ml 1.189 ml 2.377 ml
10 mM 0.119 ml 0.594 ml 1.189 ml
50 mM 0.024 ml 0.119 ml 0.238 ml
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