Azacitidine (5-Azacytidine)

製品コードS1782 バッチS178209

印刷

化学情報

Chemical Structure Synonyms 5-AzaC,Ladakamycin, AZA,5-Aza, CC-486,NSC 102816,5-Azacytidine Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C8H12N4O5
分子量 244.2 CAS No. 320-67-2
Solubility (25°C)* 体外 DMSO 49 mg/mL (200.65 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 Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
in vitro

Azacitidine (5-Azacytidine) is widely used to demonstrate the correlation between loss of methylation in specifc gene regions and activation of the associated genes. After incorporation into DNA, it inhibits DNA methyltransferase noncompetitively, causing a block in cytosine methylation in newly replicated DNA but not in resting, nondividing cells. [1] This compound induces differentiation of Friend Erythroleukemia Cell C3H10T1/2 with myotube formation. [2] It can be activated to the nucleoside triphosphate and incorporate into both DNA and RNA, leading to inhibition of DNA, RNA and protein synthesis in normal eukaryotic cells and in cancer cell lines, which could finally leads to cell death. Azacitidine also inhibits the incorporation of purine metabolites into macromolecules. It inhibits the L1210 cells growth with IC50 and of 0.019 μg/mL. [3]
in vivo

Azacitidine (5-Azacytidine) inhibits polynucleotide synthesis in leukemic BDF1 mice. [3] This compound (3 mg/kg, i.p.) increases the mean survival time in leukemic BDF1 mice inoculated with Ll210 ascites tumor cells. It markedly suppresses all enzymes activity in the polyamine-biosynthetic pathway, including ornithine decarboxylase activity. putrescine-dependent S-adenosyl-L-methionine decarboxylase activity, and spermidine-dependent S-adenosyl-L-methionine decarboxylase activity. Azacitidine also inhibits the accumulations of polyamines in leukemic mice. [4]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Leukemia L1210 cell
濃度 0.15 μg/mL
反応時間 3 days
実験の流れ

Azacitidine (5-Azacytidine) is incubated with 5 mL of L1210 cells (5 × 103 cells/mL) at 37 ℃ for 3 days. Cell number is determined twice a day for 3 days by means of a Model A Coulter counter.
動物実験 動物モデル BDF1 mice bearing lymphoid leukemia L1210
投薬量 3 mg/kg
投与方法 Daily i.p. injection

参考

  • https://pubmed.ncbi.nlm.nih.gov/12154409/
  • https://pubmed.ncbi.nlm.nih.gov/6173384/
  • https://pubmed.ncbi.nlm.nih.gov/5487063/
  • https://pubmed.ncbi.nlm.nih.gov/4118428/

カスタマーフィードバック

, , Cell, 2018, 172(1-2):90-105

Data from [Data independently produced by , , Epigenetics, 2015, 10(5): 431-45]

Data from [Data independently produced by , , Leuk Res, 2017, 58:91-97]

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：

Co-targeting of epigenetic regulators and BCL-XL improves efficacy of immune checkpoint blockade therapy in multiple solid tumors [ Mol Cancer, 2025, 24(1):154] PubMed: 40442785
A patient-derived T cell lymphoma biorepository uncovers pathogenetic mechanisms and host-related therapeutic vulnerabilities [ Cell Rep Med, 2025, S2666-3791(25)00102-8] PubMed: 40147445
ONC213: a novel strategy to resensitize resistant AML cells to venetoclax through induction of mitochondrial stress [ J Exp Clin Cancer Res, 2025, 44(1):10] PubMed: 39780285
Dual targeting of CDK6 and LSD1 is synergistic and overcomes differentiation blockade in AML [ EMBO Mol Med, 2025, 10.1038/s44321-025-00296-2] PubMed: 40883610
Glycerophospholipid metabolism licenses IgE-mediated mast cell degranulation [ Cell Rep, 2025, 44(6):115742] PubMed: 40397574
Unlocking the potential of TIGIT in enhancing therapeutic strategies for acute myeloid leukemia through combined azacitidine therapy [ NPJ Precis Oncol, 2025, 9(1):142] PubMed: 40374899
The integrative genomic and functional immunological analyses of colorectal cancer initiating cells to modulate stemness properties and the susceptibility to immune responses [ J Transl Med, 2025, 23(1):193] PubMed: 39962504
Downregulation of ECRG4 by DNMT1 promotes EC growth via IRF3/IFN-γ/miR-29b/DNMT1/ECRG4 positive feedback loop [ iScience, 2025, 28(1):111614] PubMed: 39834855
IL-17A Induces Circadian Disruptions Through the Epigenetic Repression of BMAL1 in Mice With Alzheimer's Disease [ J Cell Mol Med, 2025, 29(7):e70546] PubMed: 40208086
Knockdown of ACC1 promotes migration and invasion of U251 glioma cells by epigenetically suppressing SDH [ Int J Oncol, 2025, 67(3)73] PubMed: 40747663

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。