噴司他丁作用機(jī)制 - Medchemexpress - MCE中國(guó)

1、Product Data SheetPentostatinCat. No.: HY-A0006CAS No.: 53910-25-1分式: CHNO分量: 268.27作靶點(diǎn): Adenosine Deaminase作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (186.38 mM)* means soluble, but saturation unknown.SolventMass1 mg

2、 5 mg 10 mgConcentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存式和期限：-80C, 6 months; -20C, 1 month。-80C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?6 個(gè)內(nèi)使，-20C 儲(chǔ)存時(shí)，請(qǐng)?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都?qǐng)先按

3、照 In Vitro 式配制澄清的儲(chǔ)備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的式助溶1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (9.32 mM); Clear solution此案可獲得 2.5 mg/mL (9.32 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100

4、L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (9.32 mM); Clear solutionPage 1 of 2 www.MedChemE此案可獲得 2.5 mg/mL (9.32 mM，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 90

5、0 L 20% 的 SBE-CD 理鹽溶液中，混合均勻。3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (9.32 mM); Clear solution此案可獲得 2.5 mg/mL (9.32 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲(chǔ)備液加到 900 L 油中，混合均勻。BIOLOGICAL ACTIVITY物活性 Pentostatin (CI-825; Deoxycoformycin)種效，不可逆的腺苷脫氨酶抑制

6、劑，Ki 值為 2.5 pM。IC & Target Ki: 2.5 pM (adenosine deaminase)體內(nèi)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.戶(hù)使本產(chǎn)品發(fā)表的科研獻(xiàn) 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