| 产品描述: | ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-xL and Bcl-w inhibitor with EC50s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research |
| 靶点: |
Bcl-2:30.3 nM (EC50);Bcl-xL:78.7 nM (EC50);Bcl-W:197.8 nM (EC50);Bcl-B:1820 nM (EC50);Bfl-1:>10 μM (EC50);Mcl-1:>10 μM (EC50);Mitophagy; BCL; Autophagy |
| 体内研究: |
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. |
| 参考文献: |
1. Konopleva M, et al. Mechanisms of apoptosis sensitivity and resistance to the BH3 mimetic ABT-737 in acute myeloid leukemia. Cancer Cell. 2006 Nov;10(5):375-88. 2. Ahamed Saleem, et al. Effect of dual inhibition of apoptosis and autophagy in prostate cancer. Prostate. 2012 Sep 1;72(12):1374-81. 3. Clerc P, et al. Polster BM.Rapid Detection of an ABT-737-Sensitive Primed for Death State in Cells Using Microplate-Based Respirometry.PLoS One. 2012;7(8):e42487. Epub 2012 Aug 3. |
| 溶解性: |
DMSO : 50 mg/mL (61.47 mM; Need ultrasonic) |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.229 ml |
6.147 ml |
12.294 ml |
| 5 mM |
0.246 ml |
1.229 ml |
2.459 ml |
| 10 mM |
0.123 ml |
0.615 ml |
1.229 ml |
| 50 mM |
0.025 ml |
0.123 ml |
0.246 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。 |