| 货号 | 11500-1mg |
| 描述 | The family of Bcl-2 proteins plays pivotal roles in either promoting or preventing apoptosis. Bcl-2 family members contain one or more of four characteristic Bcl-2 homology (BH) domains, which are crucial for function. For example, anti-apoptotic Bcl-2 family proteins prevent death signaling by heterodimerizing with pro-death proteins at their BH3 domains.1 ABT-263 is a potent, orally bioavailable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki< 1 nM for all three proteins).2 It blocks the interaction of these proteins with pro-death proteins, like Bim, leading to apoptosis.2,1 ABT-263, alone, can induce regression of some tumors in some xenograft mouse models of cancer.2,3 It can also potentiate the therapeutic efficacy of chemotherapeutic compounds.2,4 Interestingly, ABT-263 induces apoptosis in cancer cell lines expressing mutants of β-catenin 1, a Wnt signaling factor commonly mutated in a range of cancer types.5 |
| 别名 | A-855071;Navitoclax; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Ni Chonghaile, T. and Letai, A. Mimicking the BH3 domain to kill cancer cells. Oncogene 27(Suppl 1), S149-S157 (2008). 2.Tse, C.,Shoemaker, A.R.,Adickes, J., et al. ABT-263: A potent and orally bioavailable Bcl-2 family inhibitor. Cancer Research 68(9), 3421-3428 (2008). 3.Shoemaker, A.R.,Mitten, M.J.,Adickes, S., et al. Activity of the Bcl-2 family inhibitor ABT-263 in a panel of small cell lung cancer xenograft models. Clinical Cancer Research 14(11), 3268-3277 (2008). 4.Wu, M.,Akinleye, A. and Zhu, X. Novel agents for chronic lymphocytic leukemia. J.Hematol.Oncol. 6, 36 (2013). 5.Basu, A.,Bodycombe, N.E.,Cheah, J.H., et al. An interactive resource to identify cancer genetic and lineage dependencies targeted by small molecules. Cell 154(5), 1151-1161 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 974.6 |
| 分子式 | C47H55ClF3N5O6S3 |
| CAS号 | 923564-51-6 |
| 稳定性 | ≥ 2 years |
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