Cidofovir dihydrate是一种无环单磷酸核苷酸类似物，一种CMV抑制剂，具有抗病毒活性。
Cas No.:113852-37-2
Sample solution is provided at 25 µL, 10mM.
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Cidofovir dihydrate is an acyclic monophosphate nucleotide analog, a CMV inhibitor, possessing antiviral activity[1-2]. Cidofovir dihydrate selectively inhibits viral DNA polymerase, thereby inhibiting cytomegalovirus replication and inducing apoptosis. Cidofovir dihydrate can be used in antiviral and cancer treatment-related research[3-4].
In vitro, MA104 cells were pretreated with Cidofovir dihydrate (50-400μM) for 6 hours, followed by infection with Human Bocavirus 1 (HBoV1) for 12 hours. Cidofovir dihydrate significantly inhibited HBoV1 replication, resulting in a dose-dependent reduction in viral DNA copy number[5]. HBoV1-HiBiTNS1-transfected HEK293T-LgBiT cells were treated with Cidofovir dihydrate (200μM) for 72 hours. Cidofovir dihydrate inhibited HBoV1 replicative activity[6].
In vivo, in an intracranial glioblastoma (GBM) xenograft mouse model, Cidofovir dihydrate (100mg/kg; intraperitoneal injection; 3 times per week) significantly extended the survival of tumor-bearing mice, induced apoptosis in tumor cells, and promoted DNA double-strand breaks while activating the p53 and Fas/TNFα-Trail pathways[7]. In a Monkeypox virus (MPXV) systemic dissemination SCID mouse model, early post-exposure administration of Cidofovir dihydrate (100mg/kg; subcutaneous injection; 2 times per week) on the day of infection or within 2 days post-infection significantly inhibited viral replication in organs such as the lungs, liver, and spleen, and alleviated histopathological damage[8].
References:
[1] Maggs DJ, Clarke HE. In vitro efficacy of ganciclovir, cidofovir, penciclovir, foscarnet, idoxuridine, and acyclovir against feline herpesvirus type-1. Am J Vet Res. 2004 Apr;65(4):399-403.
[2] Bray M, Martinez M, Smee DF, et al. Cidofovir protects mice against lethal aerosol or intranasal cowpox virus challenge. J Infect Dis. 2000 Jan;181(1):10-9.
[3] Kendle JB, Fan-Havard P. Cidofovir in the treatment of cytomegaloviral disease. Ann Pharmacother. 1998 Nov;32(11):1181-92.
[4] Stafford A, Rimmer S, Gilchrist M, et al. Use of cidofovir in a patient with severe mpox and uncontrolled HIV infection. Lancet Infect Dis. 2023 Jun;23(6):e218-e226.
[5] Tang J, Chen S, Deng Y, et al. MA104 cell line is permissive for human bocavirus 1 infection. J Virol. 2025 Feb 25;99(2):e0153924.
[6] Tang J, Chen S, Zhong Y, et al. Development of a reporter HBoV1 strain for antiviral drug screening and life cycle studies. Virol Sin. 2025 Apr;40(2):275-283.
[7] Hadaczek P, Ozawa T, Soroceanu L, et al. Cidofovir: a novel antitumor agent for glioblastoma. Clin Cancer Res. 2013 Dec 1;19(23):6473-83.
[8] Cao X, Shi N, Qiu X, et al. Intervention timing and disease stage shape tecovirimat and cidofovir efficacy in male SCID mice. Nat Commun. 2025 Dec 18;17(1):843.
Cidofovir dihydrate是一种无环单磷酸核苷酸类似物，一种CMV抑制剂，具有抗病毒活性[1-2]。Cidofovir dihydrate可通过选择性抑制病毒DNA聚合酶来抑制巨细胞病毒复制，诱导细胞凋亡。Cidofovir dihydrate可用于抗病毒、治疗癌症的相关研究[3-4]。
在体外，Cidofovir dihydrate（50-400μM）预处理MA104细胞的MA104细胞6小时，随后使用埃博拉1型病毒（HBoV1）感染细胞12小时。Cidofovir dihydrate显著抑制HBoV1复制，其病毒DNA拷贝数呈现剂量依赖性减少[5]。Cidofovir dihydrate（200μM）处理HBoV1-HiBiTNS1转染的HEK293T-LgBiT细胞72小时，Cidofovir dihydrate可抑制HBoV1复制活性[6]。
在体内，在颅内胶质母细胞（GBM）异种移植小鼠模型中，Cidofovir dihydrate（100mg/kg；腹腔注射；每周3次）显著延长了荷瘤小鼠的生存期，诱导肿瘤细胞凋亡，促进DNA双链断裂和激活p53、Fas/TNFα-Trail通路[7]。在猴痘病毒（MPXV）全身播散SCID小鼠模型中，Cidofovir dihydrate（100mg/kg；皮下注射；每周2次）在暴露后早期（感染当天或感染后2天内）给药，可显著抑制病毒在肺、肝、脾等器官的复制，并减轻组织病理损伤[8]。
| Cell experiment [1]: | |
Cell lines | MA104 cells (monkey kidney epithelial cell line) |
Preparation Method | MA104 cells were maintained in Dulbecco's modified Eagle's medium (DMEM) supplemented with 10% fetal bovine serum (FBS) at 37°C, 5% CO₂. For antiviral evaluation, MA104 cells in 12-well plates were treated with Cidofovir dihydrate (400µM, 200µM, 100µM, 50µM) for 6 hours before infection and then incubated with Human Bocavirus 1 (HBoV1) for 12 hours. After infection, cells were washed and cultured in fresh medium with or without Cidofovir dihydrate for the indicated duration. |
Reaction Conditions | 50-400μM; 6h pretreatment. |
Applications | Cidofovir dihydrate treatment resulted in a dose-dependent reduction in intracellular HBoV1 DNA copies compared to the untreated control. |
| Animal experiment [2]: | |
Animal models | Athymic nu/nu mice (homozygous) |
Preparation Method | Female athymic mice (5-6 weeks old) received intracerebral injection of 300,000 U87MG or SF7796 glioblastoma (GBM) cells into the right striatum to establish intracranial xenograft tumors. Mice were treated intraperitoneally (i.p.) with Cidofovir dihydrate at 100mg/kg, 3 times per week. Bioluminescence imaging was used to monitor tumor growth. |
Dosage form | 100mg/kg; i.p.; 3 times/week. |
Applications | Cidofovir dihydrate treatment significantly delayed or prevented intracranial GBM tumor development, as evidenced by reduced bioluminescence signal, and significantly extended the survival of tumor-bearing mice compared to the vehicle-only control group. In tumors, Cidofovir dihydrate induced extensive apoptosis, and promoted DNA double-stranded breaks. |
References: | |
| Cas No. | 113852-37-2 | SDF | |
| 别名 | 西多福韦; GS 0504; HPMPC; (S)-HPMPC | ||
| 化学名 | [(2S)-1-(4-amino-2-oxopyrimidin-1-yl)-3-hydroxypropan-2-yl]oxymethylphosphonic acid | ||
| Canonical SMILES | C1=CN(C(=O)N=C1N)CC(CO)OCP(=O)(O)O | ||
| 分子式 | C8H14N3O6P | 分子量 | 279.19 |
| 溶解度 | ≥ 13.95mg/mL in Water with gentle warming | 储存条件 | Store at -20°C |
| General tips | 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；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 3.5818 mL | 17.909 mL | 35.8179 mL |
| 5 mM | 716.4 μL | 3.5818 mL | 7.1636 mL |
| 10 mM | 358.2 μL | 1.7909 mL | 3.5818 mL |
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动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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2.
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