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dBET6
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
dBET6图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
dBET6是一种高效的,选择性的,细胞透过的基于PROTAC技术的BET降解剂,IC50值为14nM,具有抗肿瘤活性。

Animal experiment:

Mice[1]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 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[1].

产品描述

dBET6 is a highly potent, selective and cell-permeable degrader of BET based on PROTAC, with an IC50 of 14 nM, and has antitumor activity.

dBET6 is a highly potent, selective and cell-permeable degrader of BET with an IC50 of 14 nM. dBET6 (100 nM) exhibits antitumor activity against T cell acute lymphoblastic leukemia (T-ALL) lines via degradation of BRD4[1].

dBET6 (7.5 mg/kg, p.o., BID) reduces the leukemic burden in a disseminated mouse model of T-ALL[1].

[1]. Winter GE, et al. BET Bromodomain Proteins Function as Master Transcription Elongation Factors Independent of CDK9 Recruitment. Mol Cell. 2017 Jul 6;67(1):5-18.e19.