| 货号 | 16706-10mg |
| 描述 | γ-Secretase is a protease complex that cleaves single-pass transmembrane proteins, such as Notch receptors and β-amyloid precursor protein (APP), within the transmembrane domain.1,2 MK-0752 is a potent, reversible inhibitor of γ-secretase, reducing the cleavage of APP to Aβ40 in human neuroblastoma SH-SY5Y cells with an IC50 value of 5 nM.3,4 It is orally bioavailable and crosses the blood-brain barrier, as orally administered MK-0752 dose-dependently reduces the generation of new amyloid β protein in the brain of rhesus monkeys.4 Through its effects on the Notch pathway, MK-0752 reduces the number of breast cancer stem cells in tumorgrafts, enhancing the efficacy of the chemotherapy drug docetaxel (Item No. 11637) in mice with breast cancer tumors.5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Andersson, E.R. and Lendahl, U. Therapeutic modulation of Notch signalling - are we there yet? Nature Reviews.Drug Discovery 13(5), 357-378 (2014). 2.Jurisch-Yaksi, N.,Sannerud, R. and Annaert, W. A fast growing spectrum of biological functions of γ-secretase in development and disease. Biochim Biophys.Acta. 1828(12), 2815-2827 (2013). 3.Matthews, C.Z. and Woolf, E.J. Determination of a novel gamma-secretase inhibitor in human plasma and cerebrospinal fluid using automated 96 well solid phase extraction and liquid chromatography/tandem mass spectrometry. Journal of Chromatography.B, Analytical Technologies in the Biomedical and Life Sciences 863(1), 36-45 (2008). 4.Cook, J.J.,Wildsmith, K.R.,Gilberto, D.B., et al. Acute γ-secretase inhibition of nonhuman primate CNS shifts amyloid precursor protein (APP) metabolism from amyloid-β production to alternative APP fragments without amyloid-β rebound. Journal of Neuroscience 30(19), 6743-6750 (2010). 5.Schott, A.F.,Landis, M.D.,Dontu, G., et al. Preclinical and clinical studies of gamma secretase inhibitors with docetaxel on human breast tumors. Clinical Cancer Research 19(6), 1512-1524 (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 | 442.9 |
| 分子式 | C21H21ClF2O4S |
| CAS号 | 471905-41-6 |
| 稳定性 | ≥ 2 years |
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