喷司他丁作用机制 - Medchemexpress - MCE中国

1、Product Data SheetPentostatinCat. No.: HY-A0006CAS No.: 53910-25-1分式: CHNO分量: 268.27作靶点: Adenosine Deaminase作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (186.38 mM)* means soluble, but saturation unknown.SolventMass1 mg

2、 5 mg 10 mgConcentration制备储备液1 mM 3.7276 mL 18.6379 mL 37.2759 mL5 mM 0.7455 mL 3.7276 mL 7.4552 mL10 mM 0.3728 mL 1.8638 mL 3.7276 mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 储存时，请在 6 个内使，-20C 储存时，请在 1 个内使。体内实验请根据您的实验动物和给药式选择适当的溶解案。以下溶解案都请先按

3、照 In Vitro 式配制澄清的储备液，再依次添加助溶剂：为保证实验结果的可靠性，澄 的储备液可以根据储存条件，适当保存；体内实验的作液，建议您现现配，当天使； 以下溶剂前显的百分 指该溶剂在您配制终溶液中的体积占；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的式助溶1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.32 mM); Clear solution此案可获得 2.5 mg/mL (9.32 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100

4、L 25.0 mg/mL 的澄 DMSO 储备液加到 400 L PEG300 中，混合均匀；向上述体系中加50 L Tween-80，混合均匀；然后继续加 450 L 理盐定容 1 mL。2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.32 mM); Clear solutionPage 1 of 2 www.MedChemE此案可获得 2.5 mg/mL (9.32 mM，饱和度未知) 的澄清溶液。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 90

5、0 L 20% 的 SBE-CD 理盐溶液中，混合均匀。3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.32 mM); Clear solution此案可获得 2.5 mg/mL (9.32 mM，饱和度未知) 的澄 溶液，此案不适于实验周 期在半个以上的实验。以 1 mL 作液为例，取 100 L 25.0 mg/mL 的澄 DMSO 储备液加到 900 L 油中，混合均匀。BIOLOGICAL ACTIVITY物活性 Pentostatin (CI-825; Deoxycoformycin)种效，不可逆的腺苷脱氨酶抑制

6、剂，Ki 值为 2.5 pM。IC & Target Ki: 2.5 pM (adenosine deaminase)体内研究 In ECP and Pentostatin (CI-825; Deoxycoformycin; 4 mg/m2, i.v.) treatment, all dogs develop granulocytopenia with500 granulocytes/L from day 4. Thrombocytopenia (20,000 platelets/L) occurs from day 7 after HCT with nadirsof 3000 to 1400

7、0 platelets/L1. Pentostatin (2 mg/kg) in combination with cordycepin (2 mg/kg) is 100% effective inthe T. evansi-infected mice. There is an increase in levels of some biochemical parameters, especially on liverenzymes, which are accompanied by histological lesions in the liver and kidneys. Pentostat

8、in individually has nocurative effect on infected groups2.PROTOCOLAnimal All recipient dogs are conditioned for transplantation by 920 cGy TBI at 7 cGy/minute using a linear accelerator. DogsAdministration 1 in group A1receive ECP administered on days 2 and 1 with TBI on day 0 and dogs in group A2re

9、ceive ECP on days6 and 5, intravenous (IV) infusion of pentostatin at a dose of 4 mg/m2 on days 4 and 3, and TBI on day 0.Donor marrow cells from DLA-nonidentical donors are aspirated under general anesthesia through needles insertedinto humeri and femora and stored in heparinized tissue culture med

10、ium at 4C for no more than 6 hours. Within 4hours of TBI, harvested marrow cells are infused IV into recipients at a median dose of 2.9 (range, 1.9 to 6.1) 108total nucleated cells (TNC)/kg. The day of marrow grafting is designated as day 0. In addition to marrow graft,recipients are given IV infusi

11、ons of peripheral blood buffy coat cells obtained by leukapheresis from the marrowdonor on days 1 and 2, at a median dose of 2.3 (range, 1.2 to 6.9) 108 TNC/kg to ensure consistent hematopoieticengraftment. MTX, at a dose of 0.4 mg/kg intravenously is used as postgrafting immunosuppression andadmini

12、stered on days +1, +3, +6 and +11, then weekly thereafter until day 102.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Sci Transl Med. 2020 May 6;12(542). pii: eaba0769. PLoS Pathog. 2020 Mar 16;16(3):e1008341. J Nanobiotechnology. 2019 Mar

13、 29;17(1):45. J Neurochem. 2019 May 23. Virulence. 2018;9(1):1509-1520.Page 2 of 3 www.MedChemESee more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Bethge WA, et al. Extracorporeal photopheresis combined with pentostatin in the conditioning regimen for canine hematopoieti

14、c cell transplantationdoes not prevent GVHD. Bone Marrow Transplant. 2014 Sep;49(9):1198-204.2. Dalla Rosa L, et al. Cordycepin (3-deoxyadenosine) pentostatin (deoxycoformycin) combination treatment of mice experimentally infected withTrypanosoma evansi. Parasitology. 2013 Apr;140(5):663-71.McePdfHeight