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My CartCAS：320-67-2
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 320-67-2 |
| Name | 5-Azacytidine |
| Molecular Formula | C8H12N4O5 |
| Molecular Weight | 244.2 |
| Solubility | Soluble in Water/DMSO ≥10mg/mL;Soluble in Ethanol ≤2mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 206-280-2 |
| MDL | MFCD00006539 |
| SMILES | OC[C@H]1O[C@@H](N2C(N=C(N)N=C2)=O)[C@H](O)[C@@H]1O |
| InChIKey | NMUSYJAQQFHJEW-KVTDHHQDSA-N |
| InChI | InChI=1S/C8H12N4O5/c9-7-10-2-12(8(16)11-7)6-5(15)4(14)3(1-13)17-6/h2-6,13-15H,1H2,(H2,9,11,16)/t3-,4-,5-,6-/m1/s1 |
| PubChem CID | 9444 |
| Target Point | Autophagy;DNA Methyltransferase |
| Passage | Autophagy;Epigenetics |
| Background | 5-Azacytidine is acytidine nucleoside analogue and a DNA methylation inhibitor that specifically inhibits DNA methylation by binding to DNA covalently trapping DNA methyltransferases. 5-Azacytidine regulates gene expression by reducing DNA methylation levels. |
| Biological Activity | 5-Azacytidine是胞苷的核苷类似物，其通过捕获 DNA甲基转移酶 特异性地抑制DNA甲基化。[1-3] |
| In Vitro | 与多种基因相关的未甲基化CpG岛在肿瘤中部分或完全甲基化，并可被5-氮杂胞苷重新激活[1]。 5-氮杂胞苷在相同浓度范围内作为朋友红白血病细胞红细胞分化的弱诱导剂，它们影响DNA甲基转移酶活性[2]。 5-氮杂胞苷抑制L1210细胞，ID50和ID90值分别为0.019和约0.15μg/ mL [3]。 |
| In Vivo | 当动物暴露于5-氮杂胞苷(100mg / kg，ip)2小时或更长时间时，TdR-3H掺入被显着抑制[3]。 |
| Cell Experiment | 将20mL细胞(约1×10 4个细胞/ mL)用螺旋盖移液到灭菌的培养管中，并在37℃下孵育过夜。在加入1mL代谢物(或培养基)之前，通过加入1mL 5-氮杂胞苷(5-azaCR)或培养基一段给定的时间(从0到240分钟)开始实验。通过Model A Coulter计数器每天测定细胞生长两次，持续3天。为了测定IDSO和ID90值，将5mL L1210细胞(5×103细胞/ mL)与药物在37℃温育3天，并测定细胞生长。 |
| Animal Experiment | 对于体内实验，用0.2mL给定浓度的5-氮杂胞苷(5-azaCR)腹膜内注射白血病小鼠(大约1×103细胞/动物)。 2小时后，通过注射0.5mL标记的代谢物(TdR-3H或UR-3H，10 /μCi/12.5μg)开始反应。 1小时后，通过颈椎骨折杀死动物(3只小鼠/组)，用肝素处理腹水，收集，合并，然后立即在Sorvall冷冻离心机Model R2C-B中以800×g离心10分钟(4℃)。 |
| Kinase Experiment | 通过将细胞悬浮于给定体积的0.05mol / LTris-HCl缓冲液(pH 7.4)中，并用Biosonik以70％最大输出进行声波提取30秒，从培养物中的LI 210细胞中分离粗无细胞提取物。在Model L Spinco超速离心机中以105，000×g离心60分钟(4℃)后收集上清液。无细胞提取物的最终蛋白质浓度约为3mg / mL。提取物用作酶的来源。测量核糖核苷酸还原酶活性。酶单位定义为以1moleole / hr的速率催化dCMP合成的量。用于测量嘧啶核苷(CR)和脱氧核苷(TdR，CdR)激酶的测定系统基本上是Chu和Fischer描述的那些。然而，通过在沸水浴中加热2分钟终止反应，并根据Bach的方法分离磷酸化衍生物。将50μl等分试样施加到1英寸的二乙氨基乙基纸盘上，然后将其置于计数小瓶中并用0.5mL 0.5mol / LPCA洗脱。 1小时后，加入12mL Diotol，测定放射性。 |
| Data Literature Source | [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. [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. [3]. Li LH，et al. Cytotoxicity and mode of action of 5-azacytidine on L1210 leukemia. Cancer Res. 1970 Nov; 30 (11) :2760-9. |
| Unit | Bottle |
| Specification | 100mg 10mM*1mL in DMSO 500mg |
It is a potent hypomethylated growth inhibitor and cytotoxic agent that inhibits DNA methyltransferase. It is also a specific compound of the cell cycle that acts on the S phase, which can be rapidly phosphorylated and incorporated into RNA, and inhibit protein synthesis by disrupting the smooth translation of nucleic acids into proteins. The synthesis of pyrimidine can also be affected by inhibiting orotic acid nucleotide decarboxylase. It is an important regulator of gene expression, gene activation and silencing. It is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by capturing DNA methyltransferase.
Examples of using this product（for reference only）
In Vivo:
Oysters :
A total of 27 oysters were randomly divided into three groups including control group, Vs group and 5-aza + Vs group. They received individually a first injection of 100 μL sterile seawater, 100 μL sterile seawater and 100 μL 5-Azacytidine (100 μmol, Solarbio life sciences, China), respectively. Subsequently, they received individually a second injection of 100 μL sterilized seawater, 100 μL V. splendidus suspension (1×109 CFU mL? 1 in sterile seawater) and 100 μL V. splendidus suspension, respectively, at 12 h after the first injection. Haemocytes from nine oysters in each group were collected at 12 h post the second injection, and three of them were pooled together as one replicate.
Reference：
Zhao Q, Wang W, Li JX, Yuan P, Liu Y, Li Y, Wang L, Song L. The DNA cytosine-5-methyltransferase 3 (DNMT3) involved in regulation of CgIL-17 expression in the immune response of oyster Crassostrea gigas. Dev Comp Immunol. 2021 Oct;123:104092. doi: 10.1016/j.dci.2021.104092. Epub 2021 Apr 3. PMID: 33819545.
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
Note：
1. The products are all for scientific research use only. Do not use it for medical, clinical diagnosis or treatment, food and cosmetics, etc. Do not store them in ordinary residential areas.
2. For your safety and health, please wear laboratory clothes, disposable gloves and masks.
3. The experimental results may be affected by many factors, after-sale service is limited to the product itself and does not involve other compensation.
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