ABT-737 is a small-molecule inhibitor of the anti-apoptotic proteins Bcl-2, Bcl-X(L) and Bcl-w, with an affinity two to three orders of magnitude more potent than previously reported compounds. Mechanistic studies reveal that ABT-737 does not directly initiate the apoptotic process, but enhances the effects of death signals, displaying synergistic cytotoxicity with chemotherapeutics and radiation. ABT-737 exhibits single-agent-mechanism-based killing of cells from lymphoma and small-cell lung carcinoma lines, as well as primary patient-derived cells, and in animal models, ABT-737 improves survival, causes regression of established tumors, and produces cures in a high percentage of the mice. ABT-737 binds to Bcl-2, Bcl-xL and Bcl-w with very high affinities (Ki <1 nM) and also shows a very high specificity over Mcl-1 and A1.
Product Details
Alternative Name: | 4-[4-[[2-(4-chlorophenyl)phenyl]methyl]piperazin-1-yl]-N-[4-[[(2R)-4-(dimethylamino)-1-phenylsulfanylbutan-2-yl]amino]-3-nitrophenyl] sulfonylbenzamide |
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Formula: | C42H45ClN6O5S2 |
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MW: | 813.4 |
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CAS: | 852808-04-9 |
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Purity: | ≥98% (HPLC) |
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Identity: | Determined by EM-MS, NMR |
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Appearance: | Yellow powder. |
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Solubility: | Soluble in DMSO (24mg/ml) or ethanol (<1mg/ml). |
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Shipping: | Ambient |
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Short Term Storage: | +4°C |
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Long Term Storage: | -20°C |
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Regulatory Status: | RUO - Research Use Only |
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