Decitabine

製品コードS1200 バッチS120013

印刷

化学情報

Chemical Structure Synonyms Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C8H12N4O4
分子量 228.21 CAS No. 2353-33-5
Solubility (25°C)* 体外 DMSO 46 mg/mL (201.56 mM)
Water (warmed with 50ºC water bath) 46 mg/mL (201.56 mM)
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
water
10.0mg/ml Taking the 1 mL working solution as an example, add 10 mg of this product to 1 ml of ddH2O, mix evenly to make it clear, The mixed solution should be used immediately for optimal results. 
* <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 Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.
in vitro

Decitabine inhibits cell growth in a dose and time-dependent manner with IC50 of approximately 438 nM and 43.8 nM for 72 hours and 96 hours exposure in HL-60 and KG1a leukemic cells, respectively. [1] A recent study shows that Decitabine exhibits high anti-proliferative and pro-apoptotic activity against anaplastic large cell lymphoma (ALCL), and inhibits [3H]–thymidine uptake in KARPAS-299 cells with EC50 of 0.49 μM. [2]
in vivo

In a ALK+ KARPAS-299 murine xenograft model, Decitabine at a dose of 2.5 mg/kg causes increased apoptosis and reduced proliferation of tumor cells, and also results in demethylation of tumor suppressor p16INK4A. [2]

プロトコル(参考用のみ)

キナーゼアッセイ DNA synthesis assay
The rate of DNA synthesis is measured by the incorporation of radioactive thymidine into DNA. HL-60 and KG1a cells are suspended in 2 mL RPMI medium containing 10% fetal serum in 6-well (35 mm diameter) dishes and incubated with different concentrations of corresponding drugs for 48 hours (drugs are added simultaneously). At 48 hours, 0.5 μCi [3H] thymidine (6.7 Ci/mmol) is added to each well and incubated for an additional 24 hours. The cells are placed on GF/C glass fiber filters (2.4 cm diameter), washed with cold 0.9% NaCl, 5% cold trichloroacetic acid and ethanol. The filters containing the DNA are then dried, placed in EcoLite scintillation liquid (ICN) and the radioactivity measured using Beckman LS 6000IC scintillation counter. The IC50 is defined as the concentration of drug that inhibits 50% of the DNA synthesis of the leukemic cell lines from the dose–response curve.
細胞アッセイ 細胞株 HL-60 and KG1a
濃度 0-500 nM
反応時間 96 hours
実験の流れ

For the growth inhibition assay, cells in log phase are placed in 5 mL of medium. Different concentrations of Decitabine are added to the medium simultaneously. Cell counts are performed at the indicated times using a model ZM Coulter Counter. The concentration that produces 50% inhibition of growth (IC50) is determined from the growth curves of the drug treated leukemic cell lines.
動物実験 動物モデル KARPAS-299 human cells are inoculated subcutaneously into the right and left flanks of the mice.
投薬量 ≤2.5 mg/kg
投与方法 Administered via i.p.

カスタマーフィードバック

Data from [Data independently produced by PLoS One, 2014, 9(5), e97719]

Data from [Data independently produced by PLoS One, 2014, 9(5), e97719]

Data from [Leuk Res, 2014, 38(3), 402-10]

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：

Genomic and transcriptomic profiling of peripheral T cell lymphoma reveals distinct molecular and microenvironment subtypes [ Cell Rep Med, 2024, 5(2):101416] PubMed: 38350451
A functional personalised oncology approach against metastatic colorectal cancer in matched patient derived organoids [ NPJ Precis Oncol, 2024, 8(1):52] PubMed: 38413740
EFNB1 levels determine distinct drug response patterns guiding precision therapy for B-cell neoplasms [ iScience, 2024, 27(1):108667] PubMed: 38155773
Targeting G9a/DNMT1 methyltransferase activity impedes IGF2-mediated survival in hepatoblastoma [ Hepatol Commun, 2024, 8(2)e0378] PubMed: 38285887
TERT promoter methylation is associated with high expression of TERT and poor prognosis in papillary thyroid cancer [ Front Oncol, 2024, 14:1325345] PubMed: 38313800
Decitabine combined with cold atmospheric plasma induces pyroptosis via the ROS/Caspase-3/GSDME signaling pathway in Ovcar5 cells [ Biochim Biophys Acta Gen Subj, 2024, 1868(6):130602] PubMed: 38513927
Uridine-cytidine kinase 2 potentiates the mutagenic influence of the antiviral β-d-N4-hydroxycytidine [ Nucleic Acids Res, 2023, 10.1093/nar/gkad1002] PubMed: 37953355
DNMT1 mediates the disturbed flow-induced endothelial to mesenchymal transition through disrupting β-alanine and carnosine homeostasis [ Theranostics, 2023, 13(13):4392-4411] PubMed: 37649604
DNMT1 mediates the disturbed flow-induced endothelial to mesenchymal transition through disrupting β-alanine and carnosine homeostasis [ Theranostics, 2023, 13(13):4392-4411] PubMed: 37649604
Targeting polycomb repressor complex 2-mediated bivalent promoter epigenetic silencing of secreted frizzled-related protein 1 inhibits cholangiocarcinoma progression [ Clin Transl Med, 2023, 13(12):e1502] PubMed: 38050190

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。