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ABT-737

CAS No. : 852808-04-9

MCE 國際站：ABT-737

產(chǎn)品活性：ABT-737 是一種 BH3 模擬物，是一種有效的 Bcl-2、Bcl-x_L 和 Bcl-w 抑制劑，EC₅₀ 分別為 30.3 nM、78.7 nM 和 197.8 nM。ABT-737 誘導(dǎo) BCL-2/BAX 復(fù)合物的破壞和 BAK 依賴性但不依賴 BIM 的內(nèi)在凋亡途徑激活。ABT-737 誘導(dǎo)自噬，并且具有用于急性髓系白血病 (AML) 研究的潛力。

研究領(lǐng)域：Apoptosis  |  Autophagy

作用靶點(diǎn)：Bcl-2 Family  |  Apoptosis  |  Autophagy  |  Mitophagy

In Vitro: ABT-737 binds BCL-2, BCL-X_L, and BCL-W with high affinity (K_i<1 nM) but binds weakly (K_i>460 nM) to other antiapoptotic BCL-2 family members, including MCL-1 and BFL-1. ABT-737 binds the BH3-binding groove of BCL-X_L and BCL-2.
ABT-737 (100 nM; 1-72 hours) induces apoptosis and synergizes with chemotherapy in HL-60 cells.
ABT-737 (5, 7.5, 10 μM; 72 hours) causes approximately 80% HCT116 cell death. The BAX knockout variant is completely resistant to ABT-737.
ABT-737 has no effect on cell cycle distribution. ABT-737 disrupts BCL-2/BAX heterodimerization and induces BAX conformational change in HL-60 leukemic cells.
ABT-737 induces a BAX/BAK-dependent impairment of maximal O₂ consumption rate in sensitive cells. Stable BCL-2 overexpression in MCF10A cells induces an ABT-737-sensitive primed for death state. ABT-737 induces dose-dependent impairment of maximal O₂ consumption rate in B-cell lymphoma cells.

In Vivo: ABT-737 (20, 30 mg/kg/day; i.p.; for 21 days) suppresses the leukemia burden by 48% and 53% at the 20 and 30 mg/kg dose levels, respectively, in four- to six-week-old CB.17 Scid mice with human leukemia KG-1 cells.
ABT-737 significantly extends survival of mice in this aggressive leukemia model.

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