• 产品描述： DT2216 是一种基于PROTAC技术的 BCL-XL 的强效选择性降解剂。DT2216 抑制各种BCL-XL依赖性白血病和癌细胞，但对血小板的毒性较小

• 靶点： BCL-XL;Apoptosis; LigandforE3Ligase; PROTACs

• 体外研究：
  DT2216 is a BCL-XL proteolysis targeting chimera (PROTAC) that targets BCL-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation. DT2216 is more potent against various BCL-XL-dependent leukemia and cancer cells but significantly less toxic to platelets than ABT263 in vitro because VHL is poorly expressed in platelets.

• 体内研究：
  In vivo, DT2216 effectively inhibits the growth of several xenograft tumors as a single agent or in combination with other chemotherapeutic agents, without causing significant thrombocytopenia

• 细胞实验： Cell lines: MOLT-4, RS4;11, NCI-H146, MDA-MB-231, PC-3, HepG2, SW620, 786-O, WI-38, HEK 293T cells Concentrations: 0.1 μM, 0.3 μM Incubation Time: 24 h Method: MOLT-4 cells are seeded in 60 mm dishes (2.5 × 106 cells in 5 mL complete cell culture medium/dish), and then treated with indicated concentrations of DT2216 or ABT263 for 24 h. Cells are lysed in 1X cell lysis buffer by subjecting them to a freeze-thaw cycle in ice-ethanol bath or by 30 min incubation on ice.

• 动物实验： Animal Models: female 5–6 week-old CB-17 SCID, CB-17 SCID-beige, NOD-SCID mice Dosages: 7.5 mg/kg, 15 mg/kg, 25 mg/kg Administration: IP

• 参考文献：
  1. Sajid Khan, et al. A selective BCL-XL PROTAC degrader achieves safe and potent antitumor activity. Nat Med. 2019 Dec;25(12):1938-1947.

• 溶解性： Soluble  in  DMSO、Ethanol

• 保存条件： -20℃

• 配置溶液浓度参考：
  

  	1mg	5mg	10mg
  1 mM	0.648 ml	3.242 ml	6.484 ml
  5 mM	0.13 ml	0.648 ml	1.297 ml
  10 mM	0.065 ml	0.324 ml	0.648 ml
  50 mM	0.013 ml	0.065 ml	0.13 ml

• 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

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本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

• pg ng μg mg g kg =
  fM pM nM μM mM M *
  nL μL mL L *