ABT-263 is an orally-available Bcl-2 family inhibitor with Ki values of < 1 nM for Bcl-2, Bcl-xL, and Bcl-w. ABT-263 disrupts key Bcl interactions with proteins such as Bim, inducing apoptosis. Despite being a Bad-like Bh3 mimetic, ABT-263 has been shown to possess cytotoxic activity and induce apoptosis based primarily on its Bcl-2 family inhibitory activity.
ABT-263 as a standalone agent has modest activity in lymphoma and myeloma xenografts, but is extremely effective in enhancing the efficacy of clinically relevant therapies such as rituxumab and bortezomib. (1)
In a panel of small cell lung cancer (SCLC) xenografts, including H146, H889, and H1963 models, ABT-263 displays excellent antitumor effects, leading to tumor regression. (2)
Technical information:
| Chemical Formula: | C47H55ClF3N5O6S3 | |
| CAS #: | 923654-51-6 | |
| Molecular Weight: | 974.61 | |
| Purity: | > 98% | |
| Appearance: | white | |
| Chemical Name: | (R)-4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)-N-((4-((4-morpholino-1-(phenylthio)butan-2-yl)amino)-3-((trifluoromethyl)sulfonyl)phenyl)sulfonyl)benzamide | |
| Solubility: | Up to 100 mM in DMSO | |
| Synonyms: | ABT-263, Navitoclax, ABT263, ABT 263 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Tse et al., ABT-263: A Potent and Orally Bioavailable Bcl-2 Family Inhibitor. Cancer Res. 2008, 68, 3421-3428. Pubmed ID: 18451170 |
| 2. | Shoemaker et al., Activity of the Bcl-2 Family Inhibitor ABT-263 in a Panel of Small Cell Lung Cancer Xenograft Models. Clin. Cancer Res. 2008, 14, 3268-3277. Pubmed ID: 18519752 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
