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喷司他丁 /Pentostatin {[allProObj[0].p_purity_real_show]}

货号：A105564 同义名： CI-825;Deoxycoformycin

Pentostatin can inhibit adenosine deaminase irreversibly with Ki of 2.5 pM, as an antineoplastic anti-metabolite used in the treatment of several forms of leukemia.

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Pentostatin 化学结构 CAS号：53910-25-1
Pentostatin 化学结构
CAS号：53910-25-1
Pentostatin 3D分子结构
CAS号：53910-25-1
Pentostatin 化学结构 CAS号：53910-25-1
Pentostatin 3D分子结构 CAS号：53910-25-1
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Pentostatin 纯度/质量文件 产品仅供科研

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Pentostatin 生物活性

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 – 100M) 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].

Pentostatin 动物研究

Dose Rat: 0.1 mg/kg, 1 mg/kg[3] (s.c.) Dog: 0.2 mg/kg[4] (i.v.) Mice: 2 mg/kg[2] (i.p.)
Administration s.c., i.v., i.p.

Pentostatin 临床研究

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 <<

Pentostatin 参考文献

[1]Bethge WA, Kerbauy FR, et al. Extracorporeal photopheresis combined with pentostatin in the conditioning regimen for canine hematopoietic cell transplantation does not prevent GVHD. Bone Marrow Transplant. 2014 Sep;49(9):1198-204.

[2]Dalla Rosa L, da Silva AS, et al. Cordycepin (3'-deoxyadenosine) pentostatin (deoxycoformycin) combination treatment of mice experimentally infected with Trypanosoma evansi. Parasitology. 2013 Apr;140(5):663-71.

[3]Shewach DS, Krawczyk SH, Acevedo OL, Townsend LB. Inhibition of adenosine deaminase by azapurine ribonucleosides. Biochem Pharmacol. 1992 Nov 3;44(9):1697-700. doi: 10.1016/0006-2952(92)90061-m. PMID: 1449528.

[4]Aldinucci D, Poletto D, Lorenzon D, Nanni P, Degan M, Olivo K, Rapanà B, Pinto A, Gattei V. CD26 expression correlates with a reduced sensitivity to 2'-deoxycoformycin-induced growth inhibition and apoptosis in T-cell leukemia/lymphomas. Clin Cancer Res. 2004 Jan 15;10(2):508-20. doi: 10.1158/1078-0432.ccr-0755-03. PMID: 14760072.

[5]Niitsu N, Yamamoto-Yamaguchi Y, Kasukabe T, Okabe-Kado J, Umeda M, Honma Y. Antileukemic efficacy of 2-deoxycoformycin in monocytic leukemia cells. Blood. 2000 Aug 15;96(4):1512-6. PMID: 10942399.

Pentostatin 实验方案

计算器
存储液制备 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

Pentostatin 技术信息

CAS号53910-25-1
分子式C11H16N4O4
分子量 268.269
别名 CI-825;Deoxycoformycin;pentostatine. brand name: Nipent.;covidarabine;PD81565;NSC 247520;NSC 218321;2′-Deoxycoformycin;DCF;CL 67310465
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(186.38 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 100 mg/mL(372.76 mM)，配合低频超声助溶
动物实验配方

Tags: Pentostatin | 53910-25-1 | CI-825 | Deoxycoformycin | CI825 | CI 825 | Adenosine Deaminase | Metabolic Enzyme/Protease | Anti-infection | Adenosine Deaminase | Antibiotic | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Pentostatin 纯度/质量文件 | Pentostatin 生物活性 | Pentostatin 动物研究 | Pentostatin 临床数据 | Pentostatin 参考文献 | Pentostatin 实验方案 | Pentostatin 技术信息

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