目錄:MedChemExpress LLC>>信號通路>> ABT-737 | MedChemExpress
| CAS | 852808-04-9 | 純度 | 99.96% |
|---|---|---|---|
| 分子量 | 813.43 | 分子式 | C??H??ClN?O?S? |
| 供貨周期 | 現(xiàn)貨 | 規(guī)格 | 10 mM * 1 mL |
| 貨號 | HY-50907 | 應用領域 | 醫(yī)療衛(wèi)生,化工,生物產業(yè),制藥/生物制藥 |
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CAS No. : 852808-04-9
MCE 國際站：ABT-737
產品活性：ABT-737 是一種 BH3 模擬物，是一種有效的 Bcl-2、Bcl-xL 和 Bcl-w 抑制劑，EC50 分別為 30.3 nM、78.7 nM 和 197.8 nM。ABT-737 誘導 BCL-2/BAX 復合物的破壞和 BAK 依賴性但不依賴 BIM 的內在凋亡途徑激活。ABT-737 誘導自噬，并且具有用于急性髓系白血病 (AML) 研究的潛力。
研究領域：Apoptosis | Autophagy
作用靶點：Bcl-2 Family | Apoptosis | Autophagy | Mitophagy
In Vitro: ABT-737 binds BCL-2, BCL-XL, and BCL-W with high affinity (Ki<1 nM) but binds weakly (Ki>460 nM) to other antiapoptotic BCL-2 family members, including MCL-1 and BFL-1. ABT-737 binds the BH3-binding groove of BCL-XL 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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