Ganciclovir (BW 759)

製品コードS1878 バッチS187805

印刷

化学情報

 Chemical Structure Synonyms RS-21592, BW-759, 2'-Nor-2'-deoxyguanosine Storage
(From the date of receipt)
3 years -20°C powder
1 years -80°C in solvent
化学式

C9H13N5O4

分子量 255.23 CAS No. 82410-32-0
Solubility (25°C)* 体外 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.

溶剤液(一定の濃度)を調合する

生物活性

製品説明 Ganciclovirは、細胞を含まないアッセイで5.2 µMのIC50を持つ猫ヘルペスウイルス1型に対する抗ウイルス薬です。
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. This compound is sufficient to induce cell death in most bystander cells cocultured with HSV-tk-expressing cells. It significantly reduces DNA synthesis in the transformed cells, whereas it has little effect on DNA synthesis in the nontransformed cells. This chemical exhibits a concentration-dependent reduction in the rate of elongation into mature DNA. It induces cell cycle arrests rather than direct chemical effect on HSVtk-transduced B16F10 melanoma cells. It 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. Its 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. The provoked DNA instability is likely to be responsible for the observed initial decline in Bcl-2 level and caspase-9/-3 activation.
in vivo Antiviral drug ganciclovir (GCV) inhibits the proliferation of microglia in experimental autoimmune encephalomyelitis (EAE). This compound attenuates neuroinflammation and does not significantly restrain the peripheral immune response.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 BV-2 cells 
濃度 --
反応時間 24 h
実験の流れ

To assess cell proliferation by thymidine incorporation, a total of 2 × 104 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 this compound 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.

動物実験 動物モデル C57BL/6 mice
投薬量 100 mg/kg
投与方法 i.p.

参考

  • https://pubmed.ncbi.nlm.nih.gov/2847285/
  • https://pubmed.ncbi.nlm.nih.gov/8665496/
  • https://pubmed.ncbi.nlm.nih.gov/3039910/
  • https://pubmed.ncbi.nlm.nih.gov/9633514/
  • https://pubmed.ncbi.nlm.nih.gov/9731497/
  • https://pubmed.ncbi.nlm.nih.gov/11948397/
  • https://pubmed.ncbi.nlm.nih.gov/24493798/

カスタマーフィードバック

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

Selleckの高級品が、幾つかの出版された研究調査結果(以下を含む)で使われた:

Cellular senescence in malignant cells promotes tumor progression in mouse and patient Glioblastoma [ Nat Commun, 2023, 14(1):441] PubMed: 36707509
The chemotherapeutic drug doxorubicin does not exacerbate p16Ink4a-positive senescent cell accumulation and cardiometabolic disease development in [ Toxicol Appl Pharm, 2023, Volume 468, 116531] PubMed: None
The chemotherapeutic drug doxorubicin does not exacerbate p16Ink4a-positive senescent cell accumulation and cardiometabolic disease development in young [ Toxicol Appl Pharm, 2023, Volume 468 116531] PubMed: None
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

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。