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Navitoclax (ABT-263)
| Product Name | Navitoclax (ABT-263) |
| Price: | Inquiry |
| Catalog No.: | CN00505 |
| CAS No.: | 923564-51-6 |
| Molecular Formula: | C47H55ClF3N5O6S3 |
| Molecular Weight: | 974.61 g/mol |
| Purity: | >=98% |
| Type of Compound: | Alkaloids |
| Physical Desc.: | Powder |
| Source: | |
| Solvent: | Chloroform, Dichloromethane, Ethyl Acetate, DMSO, Acetone, etc. |
| SMILES: | Clc1ccc(cc1)C1=C(CN2CCN(CC2)c2ccc(cc2)C(=O)NS(=O)(=O)c2ccc(c(c2)S(=O)(=O)C(F)(F)F)N[C@@H](CSc2ccccc2)CCN2CCOCC2)CC(CC1)(C)C |
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| Description | Navitoclax (ABT-263) is a potent and oral 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. |
| Target | Bcl-W:1 nM (Ki) Bcl-xL:1 nM (Ki) Bcl-2:1 nM (Ki) |
| In Vitro | 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 at all paclitaxel doses tested in both SK-OV-3 and IGROV-1 cell lines[2]. |
| In Vivo | Navitoclax (100 mg/kg/day, p.o.) also improves responses to bendamustine-rituximab (BR) in a subset of tumours in mice xenograft[3]. |
| Cell Assay | Cells are seeded in 384-well plates at 3,000 cells per well. After 24 hours, cells are treated with navitoclax (dose range of 14 nM-3.3 μM) and paclitaxel (dose range of 15 pM-100 nM) or gemcitabine (dose range of 0.5 nM-3.3 μM) in a 9 by 7 matrix. Each treatment is carried out in quadruplicate. Cells are treated for 72 hours, and cell viability is determined using the CellTiter-Glo assay. Cell viability for each treatment is normalized against the DMSO control group. |
| Animal Admin | For systemic Granta 519 tumour models, 2×106 cells are injected via the tail vein in 0.1 mL volume of cell medium on day 0, and treatment is initiated on day 14. All animals are ear-tagged and monitored individually throughout the experiment. Navitoclax is administered by oral gavage once daily in a mixture of Phosal 50PG : PEG400 : ethanol. Bendamustine and rituximab are administered i.v. at 25 and 10 mg/kg, respectively, on day 1. Navitoclax is administered approximately 2 h before bendamustine and rituximab. All trials are comprised of 10 mice per group. Mice are humanely killed when tumours reached a size >2000 mm3 or when any signs of distress are monitored. Signs of distress include loss of ambulation, laboured breathing or weight loss > 20% mean body weight per cage. |
| Density | 1.4±0.1 g/cm3 |
| Exact Mass | 973.295532 |
| PSA | 170.42000 |
| LogP | 12.14 |
| Storage condition | -20°C Freezer, Under Inert Atmosphere |