产品说明书

Ganciclovir

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Chemical Structure| 82410-32-0 同义名 : 更昔洛韦 ;BW 759;2'-Nor-2'-deoxyguanosine;2'-Nor-2'-deoxyguanosine, BW 759, Ganciclovir;RS-21592
CAS号 : 82410-32-0
货号 : A200267
分子式 : C9H13N5O4
纯度 : 98%
分子量 : 255.231
MDL号 : MFCD00870588
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(235.08 mM)，配合低频超声助溶，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: 1.5 mg/mL(5.88 mM)，配合低频超声助溶
动物实验配方：

4% DMSO+30% PEG 300+water 2 mg/mL

生物活性
描述 Ganciclovir, a guanosine nucleoside analogue, is a well established broad-spectrum antiviral agent that inhibits replication of viral DNA and is active against both HSV-1 and -2 and several other viruses. Ganciclovir ophthalmic gel 0.15% is a five-times-daily topical preparation that is indicated for the treatment of acute herpetic keratitis (dendritic ulcers). Ganciclovir ophthalmic gel 0.15% was generally well tolerated and was associated with a significantly lower incidence of visual disturbances than aciclovir ointment 3% in the phase III trial[3]. TFT (trifluorothymidine) and GCV (Ganciclovir) are synergistic against acyclovir-susceptible HSV-1 at concentrations significantly less toxic than if each antiviral were used as a sole agent[4]. GCV is used as an antiviral drug, and the thymidine kinase, HSV‑TK can phosphorylate GCV to GCV‑TP, a competitive inhibitor of DNA synthesis, instead of guanine‑5'‑triphosphate in the process of DNA synthesis. HSV‑TK/GCV (Herpes simplex virus type 1 thymidine kinase/ganciclovir) can significantly cause the death of retinoblastoma cell lines, HXO‑RB44 and Y79[5]. When HSV-Tk(+) T cells are added to T cell-depleted BM a consequently developing GVH can be controlled by GCV treatment with 60-70% of the animals surviving[6]. Moreover, long-circulating liposome-encapsulated GCV is a new approach to drug carriers to enhance the efficacy of suicide gene therapy[7].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
BSC-1 cells Function assay Antiviral activity of the compound was evaluated against the Herpes simplex virus type-1 in BSC-1 cells, IC50=3 μM 2913300
CEM cells Cytotoxic assay Cytotoxicity against CEM cells, CC50=5 μM 15615545
E6SM cell lines Function assay Effective concentration required to inhibit Herpes simplex virus-2 (HSV-2) induced cytopathicity by 50% in E6SM cell lines, EC50=1.2 nM 11495586
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
NCT01663740 Cytomegalovirus Infections Phase 4 Completed - United States, California ... 展开 >> National Institute of Transplantation Los Angeles, California, United States, 90057 University of California Los Angeles (UCLA) Los Angeles, California, United States, 90095 University of California at San Francisco San Francisco, California, United States, 94115 United States, District of Columbia Washington Hospital Center Washington, District of Columbia, United States, 20010 United States, Georgia Medical College of Georgia Augusta, Georgia, United States, 30912 United States, Massachusetts Tufts Medical Center Boston, Massachusetts, United States, 02111 Western New England Renal & Transplant Associates, P.C. Springfield, Massachusetts, United States, 01107 United States, Minnesota University of Minnesota Minneapolis, Minnesota, United States, 55455 Mayo Clinic Rochester Rochester, Minnesota, United States, 55902 United States, New York Albany Medical Cancer Center Albany, New York, United States, 12208 University at Buffalo Buffalo, New York, United States, 14203 Stony Brook University Hospital Stony Brook, New York, United States, 11794 United States, Oregon Oregan Health & Science Univ Portland, Oregon, United States, 97237 United States, Pennsylvania Drexel University Department of Nephrology Philadelphia, Pennsylvania, United States, 19102 United States, Rhode Island Rhode Island Hospital Providence, Rhode Island, United States, 02903 United States, Texas Methodist Healthcare System of San Antonio San Antonio, Texas, United States, 78229 Mexico Hospital Miguel Hidalgo Aguascalientes, Mexico, 20230 Instituto Mexicano de Trasplantes Cuernavaca, Mexico, 62448 Hospital Central Dr. Ignacio Morones Prieto San Luis Potosi, Mexico, 78240 收起 <<
NCT00005025 Fallopian Tube Cancer ... 展开 >> Ovarian Cancer Primary Peritoneal Cavity Cancer 收起 << Phase 2 Unknown - United States, Iowa ... 展开 >> Human Gene Therapy Research Institute Des Moines, Iowa, United States, 50309 收起 <<
NCT02202564 Liver Cancer ... 展开 >>Hepatocellular Carcinoma 收起 << Phase 2 Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.92mL

0.78mL

0.39mL

19.59mL

3.92mL

1.96mL

39.18mL

7.84mL

3.92mL
参考文献

[1]Tomicic MT, Thust R, Kaina B. Ganciclovir-induced apoptosis in HSV-1 thymidine kinase expressing cells: critical role of DNA breaks, Bcl-2 decline and caspase-9 activation. Oncogene. 2002 Mar 28;21(14):2141-53.

[2]Hamel W, Magnelli L, et al. Herpes simplex virus thymidine kinase/ganciclovir-mediated apoptotic death of bystander cells. Cancer Res. 1996 Jun 15;56(12):2697-702.

[3]Croxtall JD. Ganciclovir ophthalmic gel 0.15%: in acute herpetic keratitis (dendritic ulcers). Drugs. 2011 Mar 26;71(5):603-10

[4]Hobden JA, Kumar M, Kaufman HE, Clement C, Varnell ED, Bhattacharjee PS, Hill JM. In vitro synergism of trifluorothymidine and ganciclovir against HSV-1. Invest Ophthalmol Vis Sci. 2011 Feb 11;52(2):830-3

[5]Yi QY, Bai ZS, Cai B, Chen N, Chen LS, Yuan T, Mao JH. HSV‑TK/GCV can induce cytotoxicity of retinoblastoma cells through autophagy inhibition by activating MAPK/ERK. Oncol Rep. 2018 Aug;40(2):682-692

[6]Weijtens M, van Spronsen A, Hagenbeek A, de Weger R, Martens A. Ganciclovir-mediated elimination of HSV-Tk+ T cells and cure of graft-vs-host disease in an allogeneic bone marrow transplantation model in the rat. Exp Hematol. 2004 Oct;32(10):962-9

[7]Kajiwara E, Kawano K, Hattori Y, Fukushima M, Hayashi K, Maitani Y. Long-circulating liposome-encapsulated ganciclovir enhances the efficacy of HSV-TK suicide gene therapy. J Control Release. 2007 Jul 16;120(1-2):104-10