货号 | 11501-1mg |
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 BH3domains.1 ABT-737 is a potent, cell-permeable mimetic of BH3 domains that avidly binds Bcl-2, Bcl-xL, and Bcl-W (Ki< 1 nM for all three proteins).2,3 It blocks the interaction of these proteins with pro-death proteins, leading to apoptosis.2 ABT-737, alone, can induce regression of some tumors in some xenograft mouse models of cancer.2,1 It shows synergy with diverse therapeutics and radiation to trigger apoptosis in cancer cells and xenografts.2,4,5 |
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.Oltersdorf, T.,Elmore, S.W.,Shoemaker, A.R., et al. An inhibitor of Bcl-2 family proteins induces regression of solid tumours. Nature 435(7042), 677-681 (2005). 3.Bruncko, M.,Oost, T.K.,Belli, B.A., et al. Studies leading to potent, dual inhibitors of Bcl-2 and Bcl-xL. Journal of Medicinal Chemistry 50(4), 641-662 (2007). 4.Trudel, S.,Stewart, A.K.,Li, Z., et al. The Bcl-2 family protein inhibitor, ABT-737, has substantial antimyeloma activity and shows synergistic effect with dexamethasone and melphalan. Clinical Cancer Research 13(2), 621-629 (2007). 5.Konopleva, M.,Watt, J.,Contractor, R., et al. Mechanisms of antileukemic activity of the novel Bcl-2 homology domain-3 mimetic GX15-070 (obatoclax). Cancer Research 68(9), 3413-3420 (2008). | |
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 | 813.4 |
分子式 | C42H45ClN6O5S2 |
CAS号 | 852808-04-9 |
稳定性 | ≥ 2 years |
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