生物活性 | |||
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描述 | Adenosine deaminase (ADA) is a critical enzyme that mediates the intracellular level of adenosine via the irreversible deamination of adenosine to inosine and thereby degrades purine and deoxypurine nucleotides. Pentostatin irreversibly inhibits ADA with a Ki value of 0.09 nM, which results in the accumulation of triphosphate metabolites in the cytosol and impedes DNA synthesis in dividing cells[3]. The treatment with pentostatin (1 – 100M) in combination with 2′-deoxyadenosine inhibited the colony growth in T-cells lacking surface CD26/ADA complex expression in a dose-dependent manner. Pentostatin at 0.5μM reduced the cell survival to 50% of control in KE-37 and FRO cell lines. It also led to a 50% survival reduction versus control at 1.0 and 11μM in Jurkat cell line and CEM cell line, respectively. Incubation of T-cell lines with pentostatin (25μM) and 2′-deoxyadenosine (25μM) increased the percentage of apoptotic nuclei and the number of apoptotic cells detected in the sub-G1 areas compared to the control group[4]. In nude mice inoculated with human monocytoid U937 cells, injection of pentostatin (0.25 and 2.5mg/kg, 3 times per week) significantly prolonged the mean survival rate (28.6 and 31.2 days, respectively) in comparison to the controls (21.5 days)[5]. |
临床研究 | |||||
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NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02551718 | Acute Leukemia of Ambiguous Li... 展开 >>neage Recurrent Adult Acute Lymphoblastic Leukemia Recurrent Adult Acute Myeloid Leukemia Recurrent Childhood Acute Lymphoblastic Leukemia Recurrent Childhood Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Refractory Adult Acute Lymphoblastic Leukemia Refractory Childhood Acute Lymphoblastic Leukemia 收起 << | Not Applicable | Recruiting | - | United States, Washington ... 展开 >> Fred Hutch/University of Washington Cancer Consortium Recruiting Seattle, Washington, United States, 98109 Contact: Pamela S. Becker 206-616-1589 pbecker@u.washington.edu Principal Investigator: Pamela S. Becker 收起 << |
NCT03663933 | Lymphoproliferative Disorders ... 展开 >> Autoimmune Lymphoproliferative Primary T-cell Immunodeficiency Disorders Immune System Diseases Common Variable Immunodeficiency 收起 << | Phase 2 | Recruiting | May 1, 2024 | United States, Maryland ... 展开 >> National Institutes of Health Clinical Center Recruiting Bethesda, Maryland, United States, 20892 Contact: For more information at the NIH Clinical Center contact National Cancer Institute Referral Office 888-624-1937 收起 << |
NCT01862965 | Chronic Graft-versus-host Dise... 展开 >>ase 收起 << | Phase 2 | Active, not recruiting | June 2018 | Germany ... 展开 >> Universitätsklinikum Hamburg-Eppendorf Hamburg, Germany, 20246 Universitätsklinikum Jena Jena, Germany, 07743 Universitätsmedizin der Johannes Gutenberg-Universität Mainz Mainz, Germany, 55101 Klinikum der Universität Regensburg Regensburg, Germany, 93053 Universitätsklinikum Ulm Ulm, Germany, 89081 Deutsche Klinik fuer Diagnostik GmbH Wiesbaden, Germany, 65191 收起 << |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.73mL 0.75mL 0.37mL |
18.64mL 3.73mL 1.86mL |
37.28mL 7.46mL 3.73mL |
参考文献 |
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