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dBET6 是一种基于 PROTAC 的选择性和细胞渗透性 BET 降解剂,IC50值为 14 nM。 它具有抗肿瘤活性。
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dBET6 是一种基于 PROTAC 的选择性和细胞渗透性 BET 降解剂,IC50值为 14 nM。 它具有抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 397 | 现货 | |
5 mg | ¥ 947 | 现货 | |
10 mg | ¥ 1,660 | 现货 | |
25 mg | ¥ 2,990 | 现货 | |
50 mg | ¥ 3,970 | 现货 | |
100 mg | ¥ 5,260 | 现货 | |
200 mg | ¥ 6,590 | 现货 | |
500 mg | ¥ 9,780 | 现货 | |
1 mL x 10 mM (in DMSO) | ¥ 1,190 | 现货 |
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. |
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) |
存储 | keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 10 mM | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
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