| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Cell lines | Murine DO11.10 T-hybridoma cells expressing murine Bcl-2, Bcl-xL and Bcl-w proteins |
Preparation method | The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. |
Reaction Conditions | None specifc suggestion |
Applications | ABT-263 is an antitumor effector in preclinical and early clinical studies. It binds to Bcl-2, Bcl-xL, and Bcl-win vitro, but only targets Bcl-2in vivo. In human non-Hodgkin lymphomas, high expression of Bcl-2 sensitized to ABT-263 elevated proapoptotic Bim. |
Animal models | Immune-deficient NOD/SCID or NOD/SCID, ILγ receptor negative mice |
Dosage form | Orally taken at 100 mg/kg/day for 21 days |
Applications | ABT-263 can largely inhibited the activity of patient-derived pediatric acute lymphoblastic leukemia xenograft. ABT-263 sensitivity was correlated with low MCL1 mRNA expression levels. BH3 profiling revealed that resistance to ABT-263 correlated with mitochondrial priming by NOXA peptide. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
| 产品描述 | Navitoclax (ABT-263) is a potent and orally active Bcl-2 family protein inhibitor that binds to multiple anti-apoptotic Bcl-2 family proteins, such as Bcl-xL, Bcl-2 and Bcl-w, with a Ki of less than 1 nM. Navitoclax (ABT-263) is active against approximately one-half of the cell lines of the PPTP in vitro panel. The median IC50 for all of the lines in the panel is 1.91 μM[1]. Navitoclax in combination with chemotherapy agents leads most ovarian cancer cell lines a synergistic response, and enhances the caspase activation in both SK-OV-3 and IGROV-1 cell lines[2]. Navitoclax (100 mg/kg; orally; 21-day treatment) enhances the activity of OSI-744 in vivo. As a single agent, 100 mg/kg Navitoclax alone dosed daily has no significant antitumor activity, whereas daily dosing of OSI-744 at 50 mg/kg results in significant tumor stasis (%TGI=52) during a 21-day treatment period. Notably, the combination of Navitoclax and OSI-744 dosed daily for 21 consecutive days results in 98% TGI and durable tumor regressions in 100% of treated tumor-bearing mice[3]. References: |
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