Ganciclovir

Catalog No.S1878 Batch:S187803

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Technical Data

Formula

C9H13N5O4
Molecular Weight 255.23 CAS No. 82410-32-0
Solubility (25°C)* In vitro DMSO 50 mg/mL (195.9 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Ganciclovir is an antiviral drug for feline herpesvirus type-1 with IC50 of 5.2 μM in a cell-free assay.
In vitro Ganciclovir is metabolized to the triphosphate form by primarily three cellular enzymes: (1) a deoxyguanosine kinase induced by CMV-infected cells; (2) guanylate kinase; and (3) phosphoglycerate kinase. [1] Ganciclovir is sufficient to induce cell death in most bystander cells cocultured with HSV-tk-expressing cells. [2] Ganciclovir significantly reduces DNA synthesis in the transformed cells, whereas Ganciclovir has little effect on DNA synthesis in the nontransformed cells. Ganciclovir exhibits a concentration-dependent reduction in the rate of elongation into mature DNA. [3] Ganciclovir induces cell cycle arrests rather than direct chemical effect on HSVtk-transduced B16F10 melanoma cells. [4] Ganciclovir produces only weak inhibition of DNA synthesis. Ganciclovir-treated cells accumulate in early S-phase and remained there until cell death, suggesting that ganciclovir incorporation in the DNA template is important for cytotoxicity. [5] Ganciclovir-induced apoptosis is due to incorporation of the drug into DNA resulting in replication-dependent formation of DNA double-strand breaks and, at later stages, S and G2/M arrest. Ganciclovir-provoked DNA instability is likely to be responsible for the observed initial decline in Bcl-2 level and caspase-9/-3 activation. [6]
In vivo Antiviral drug ganciclovir (GCV) inhibits the proliferation of microglia in experimental autoimmune encephalomyelitis (EAE). GCV attenuates neuroinflammation and does not significantly restrain the peripheral immune response[7].

Protocol (from reference)

Cell Assay:

[7]
  • Cell lines

    BV-2 cells 

  • Concentrations

    --

  • Incubation Time

    24 h

  • Method

    To assess cell proliferation by thymidine incorporation, a total of 2 × 10<sup>4</sup> BV-2 cells were seeded in a 96-well plate for a maximum of 12 h in 10% FBS containing DMEM and then serum starved for an additional 12 h before the addition of varying concentrations of GCV for a total of 24 h. Cultures were pulsed for the final 8 h with 1 µCi/well [3H]thymidine before incorporated radioactivity was measured using a β plate scintillation counter.
Animal Study:

[7]
  • Animal Models

    C57BL/6 mice

  • Dosages

    100 mg/kg

  • Administration

    i.p.

Customer Product Validation

Data from [Data independently produced by , , Sci Rep, 2017, 7: 43349]

Selleck's Ganciclovir has been cited by 16 publications

Cellular senescence in malignant cells promotes tumor progression in mouse and patient Glioblastoma [ Nat Commun, 2023, 14(1):441] PubMed: 36707509
Effects of cancer-associated fibroblasts deletion using HSVtk suicide system in OSCC [ Oral Dis, 2023, 10.1111/odi.14612] PubMed: 37203377
Tumor perivascular cell-derived extracellular vesicles promote angiogenesis via the Gas6/Axl pathway [ Cancer Lett, 2022, 524:131-143] PubMed: 34678434
Senescent hepatic stellate cells promote liver regeneration through IL-6 and ligands of CXCR2 [ JCI Insight, 2022, 7(14)e158207] PubMed: 35708907
Dioscin potentiates the antitumor effect of suicide gene therapy in melanoma by gap junction intercellular communication-mediated antigen cross-presentation [ Biomed Pharmacother, 2022, 150:112973] PubMed: 35468581
Safety, efficacy and delivery of multiple nucleoside analogs via drug encapsulated carbon (DECON) based sustained drug release platform [ Eur J Pharm Biopharm, 2022, S0939-6411(22)00047-9] PubMed: 35314347
Pericytes augment glioblastoma cell resistance to temozolomide through CCL5-CCR5 paracrine signaling [ Cell Res, 2021, 10.1038/s41422-021-00528-3] PubMed: 34239070
NUDT15-mediated hydrolysis limits the efficacy of anti-HCMV drug ganciclovir [ Cell Chem Biol, 2021, S2451-9456(21)00268-3] PubMed: 34192523
TGF-β/Alk5 signaling prevents osteoarthritis initiation via regulating the senescence of articular cartilage stem cells [ J Cell Physiol, 2021, 10.1002/jcp.30231] PubMed: 33452687
6-Thioguanine Inhibits Herpes Simplex Virus 1 Infection of Eyes [ Microbiol Spectr, 2021, 9(3):e0064621] PubMed: 34730435

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.