5-Azacytidine (Synonyms: 5-氮雜胞苷; Azacitidine; 5-AzaC; Ladakamycin)
5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) 是胞苷核苷類似物，特異型抑制 DNA 甲基化。5-Azacytidine 與 DNA 結合共價捕獲 DNA甲基轉移酶 (DNA methyltransferases)，有益于逆轉表觀遺傳變化。5-Azacytidine 誘導細胞自噬 (autophagy)。
生物活性
5-Azacytidine (Azacitidine; 5-AzaC; Ladakamycin) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation. 5-Azacytidine is incorporated into DNA to covalently trap DNA methyltransferases and contributes to reverse epigenetic changes[1][2]. 5-Azacytidine induces cell autophagy[4].
IC50 & Target[1]
DNMT1 Nucleoside Antimetabolite/Analog Autophagy
體外研究(In Vitro)
Unmethylated CpG islands associated with a variety of genes become partially or fully methylated in tumors and can be reactivated by 5-Azacytidine[1]. 5-Azacytidine acts as weak inducers of erythroid differentiation of Friend erythroleukemia cells in the same concentration range where they affect DNA methyltransferase activity[2]. 5-Azacytidine inhibits L1210 cells with ID50 and ID90 values of 0.019 and circa 0.15 μg/mL, respectively[3].
體內研究(In Vivo)
TdR-3H incorporation is significantly inhibited when the animals are exposed to 5-Azacitidine (100 mg/kg, i.p.) for 2 hr or longer[3].
分子量：244.20
Formula：C8H12N4O5
CAS 號：320-67-2
中文名稱：阿扎胞苷；阿托胞苷；5-氮包苷；5-氮雜胞苷；5-氮雜胞嘧啶核苷；氮胞苷；氮雜胞苷
運輸條件
Room temperature in continental US; may vary elsewhere.
儲存方式
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
溶解性數據
In Vitro:
H2O : 33.33 mg/mL (136.49 mM; Need ultrasonic)
DMSO : ≥ 31 mg/mL (126.95 mM)
* "≥" means soluble, but saturation unknown.
| 濃度溶劑體積質量 | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 4.0950 mL | 20.4750 mL | 40.9500 mL |
| 5 mM | 0.8190 mL | 4.0950 mL | 8.1900 mL |
| 10 mM | 0.4095 mL | 2.0475 mL | 4.0950 mL |
請根據產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內使用，-20°C 儲存時，請在 1 個月內使用。
以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據儲存條件，適當保存；體內實驗的工作液，建議您現用現配，當天使用； 以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現沉淀、析出現象，可以通過加熱和/或超聲的方式助溶
- 1.
請依序添加每種溶劑： PBS
Solubility: 20 mg/mL (81.90 mM); Clear solution; Need ultrasonic
- 2.
請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution
- 3.
請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution
- 4.
請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.52 mM); Clear solution
參考文獻
[1]. Christman JK. 5-Azacytidine and 5-aza-2'-deoxycytidine as inhibitors of DNA methylation: mechanistic studies and their implications for cancer therapy. Oncogene. 2002 Aug 12;21(35):5483-95. Content Brief
[2]. Creusot F, et al. Inhibition of DNA methyltransferase and induction of Friend erythroleukemia cell differentiation by 5-azacytidineand 5-aza-2'-deoxycytidine. J Biol Chem. 1982 Feb 25;257(4):2041-8. Content Brief
[3]. Li LH,et al. Cytotoxicity and mode of action of 5-azacytidine on L1210 leukemia. Cancer Res. 1970 Nov;30(11):2760-9. Content Brief
[4]. Marycz K, et al. 5-Azacytidine and Resveratrol Enhance Chondrogenic Differentiation of Metabolic Syndrome-Derived Mesenchymal Stem Cells by Modulating Autophagy.Oxid Med Cell Longev. 2019 May 12;2019:1523140. Content Brief
注:產品僅用于科研
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