规格

价格

库存

数量

1 mg

¥ 292

现货

5 mg

¥ 695

现货

10 mg

¥ 1,190

现货

25 mg

¥ 2,160

现货

50 mg

¥ 2,900

现货

100 mg

¥ 3,820

现货

1 mL x 10 mM (in DMSO)

¥ 866

现货

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) 通过降解BRD4，展现出对T细胞急性淋巴细胞性白血病（T-ALL）细胞株的抗肿瘤活性。
体内活性	dBET6 (7.5 mg/kg, p.o., BID) 在分散型T-ALL小鼠模型中降低了白血病负荷。
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 No.	1950634-92-0
Smiles	CC=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
密度	1.48 g/cm3 (Predicted)

储存&溶解度

存储

keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 112.5 mg/mL (133.71 mM), Sonication is recommended.

体内实验配方

10% DMSO+90% Corn Oil: 1 mg/mL (1.19 mM), Sonication is recommeded.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

DMSO