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更昔洛韦 /Ganciclovir {[allProObj[0].p_purity_real_show]}

货号:A200267 同义名: 更昔洛韦 / BW 759;2'-Nor-2'-deoxyguanosine

Ganciclovir(BW 759)是一种核苷类似物,是口服活性抗病毒剂,对CMV巨细胞病毒)有活性。更昔洛韦在体外也对疱疹病毒组的一些成员及其他一些DNA病毒有活性。更昔洛韦抑制人类疱疹病毒(HSV 1和2,CMV)和腺病毒1、2、4、6、8、10、19、22和28型的体外复制。更昔洛韦对猫疱疹病毒1型(FHV-1)的IC50为5.2 μM,并能扩散到脑内。

HazMat Fee +

There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.

Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Ganciclovir 化学结构 CAS号:82410-32-0
Ganciclovir 化学结构
CAS号:82410-32-0
Ganciclovir 3D分子结构
CAS号:82410-32-0
Ganciclovir 化学结构 CAS号:82410-32-0
Ganciclovir 3D分子结构 CAS号:82410-32-0
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Ganciclovir 纯度/质量文件 产品仅供科研

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Ganciclovir 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].

Ganciclovir 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
HEL cells Function assay Antiviral activity against HSV1 KOS infected in HEL cells assessed as inhibition of virus-induced cytopathic effect, EC50=10 nM 21232828

Ganciclovir 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 - -

Ganciclovir 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

Ganciclovir 实验方案

计算器
存储液制备 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

Ganciclovir 技术信息

CAS号82410-32-0
分子式C9H13N5O4
分子量 255.231
别名 更昔洛韦 ;BW 759;2'-Nor-2'-deoxyguanosine;2'-Nor-2'-deoxyguanosine, BW 759, Ganciclovir;RS-21592
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,2-8°C

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

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