常用名：DT2216

产品描述：

DT2216 inhibits various Bcl-XL-dependent leukemias and cancer cells, but is significantly less toxic to platelets.DT2216 is a selective B-cell lymphoma, extremely large (BCL-XL), proteolytic targeting chimera (PROTAC).DT2216 targets bcl-XL to the Von Hippel-Lindau (VHL) E3 ligase for degradation.

体外活性 DT2216 (0.1, 0.3 μM; 24 hours) kills MOLT-4 cells by caspase-3-mediated induction of apoptosis in a BCL-2 homologous antagonist killer (BAK)- and BCL-2-associated X protein (BAX)-dependent manner.DT2216 (62.5, 125 nM; 72?hours) kills MOLT-4 cells. DT2216 (0.001-10 μM; 72?hour) shows highly toxic to MOLT-4 cells with an EC50 of 0.052 μM.

体内活性 DT2216 (i.p.; 7.5, 15 mg/kg; weekly for 60 days) of 15 mg/kg is more effective at suppressing the growth of MOLT-4 T-ALL xenografts in mice than 7.5 mg/kg.

分子量 1542.36

分子式 C77H96ClF3N10O10S4

CAS No. 2365172-42-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 25 mg/mL (16.21 mM), Sonication is recommended.

H2O: < 0.1 mg/mL (insoluble)

PROteolysis TArgeting Chimeras (PROTACs) 通过将靶蛋白和 E3 连接酶结合起来，从而“劫持”细胞的泛素-蛋白酶体系统（UPS）来实现蛋白质的降解。由于 PROTACs 只需具有高选择性地结合其靶标（而不是抑制靶蛋白的酶活性），目前有许多努力将先前无效的抑制剂分子改造为 PROTACs，用作下一代药物。

产地：西安

用途：科研！

厂家：西安齐岳生物科技有限公司

温馨提示：仅用于科研，不能用于人体实验！

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