DT2216 抑制各种 BCL-XL 依赖性白血病和癌细胞，但对血小板的毒性显着降低。DT2216 是一种选择性 B 细胞淋巴瘤，极大 (BCL-XL)，蛋白水解靶向嵌合体 (PROTAC)。DT2216 靶向 BCL-XL到 Von Hippel-Lindau (VHL) E3 连接酶进行降解。

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.

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.

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.

2365172-42-3

C77H96ClF3N10O10S4

1542.36

H2O:< 0.1 mg/mL (insoluble)
DMSO:25 mg/mL (16.21 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years