5-Azacytidine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
5-Azacytidine(5-AzaC),属于胞嘧啶类似物的化合物,是DNA甲基转移酶(DNMT)的抑制剂,对多发性骨髓瘤(MM)细胞,包括MM.1S、MM.1R、RPMI-8266、RPMI-LR5、RPMI-Dox40和患者来源的MM具有有效的细胞毒性,IC50值分别为1.5 μmol/L、0.7 μmol/L、1.1 μmol/L、2.5 μmol/L、3.2 μmol/L和1.5 μmol/L[1]。
5-Azacytidine可插入到细胞的DNA和/或RNA上,随后螯合DNMT,在5-Azacytidine的C6和DNMTs的半胱氨酸硫醇之间形成共价键,导致细胞中DNMT活性的缺失和DNA去甲基化[1]。
参考文献:
[1] Kiziltepe T, Hideshima T, Catley L, Raje N, Yasui H, Shiraishi N, Okawa Y, Ikeda H, Vallet S, Pozzi S, Ishitsuka K, Ocio EM, Chauhan D, Anderson KC. 5-Azacytidine, a DNA methyltransferase inhibitor, induces ATR-mediated DNA double-strand break responses, apoptosis, and synergistic cytotoxicity with doxorubicin and bortezomib against multiple myeloma cells. Mol Cancer Ther. 2007 Jun;6(6):1718-27.
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Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 244.2 |
Cas No. | 320-67-2 |
Formula | C8H12N4O5 |
Solubility | insoluble in EtOH; ≥24.45 mg/mL in DMSO; ≥13.55 mg/mL in H2O with ultrasonic |
Chemical Name | 4-amino-1-[(2R,3R,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-1,3,5-triazin-2-one |
SDF | Download SDF |
Canonical SMILES | C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
白血病L1210细胞 |
制备方法 |
在DMSO中的溶解度大于12.2 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37°C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20°C可放置数月。 |
反应条件 |
80 μM;0~120分钟 |
实验结果 |
在白血病L1210细胞中,相对于RNA合成,5-Azacytidine对DNA合成的抑制作用更大。经过90分钟预孵育后,TdR-3H掺入被抑制了约74%,而UR-3H掺入被抑制了仅仅32%。 |
动物实验 [2]: | |
动物模型 |
携带淋巴性白血病L1210细胞的BDF1小鼠 |
给药剂量 |
3 mg/kg;腹腔注射;每天1次 |
实验结果 |
在携带淋巴性白血病L1210细胞的BDF1小鼠中,5-Azacytidine增加了平均存活时间。此外,5-Azacytidine显著抑制多胺生物合成途径中的所有酶的活性。此外,5-Azacytidine抑制多胺在白血病小鼠中的积累。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: [1]. Li LH, Olin EJ, Buskirk HH, Reineke LM. Cytotoxicity and mode of action of 5-azacytidine on L1210 leukemia. Cancer Res. 1970 Nov;30(11):2760-9. [2]. Heby O, Russell DH. Depression of polyamine synthesis in L1210 leukemic mice during treatment with a potent antileukemic agent, 5-azacytidine. Cancer Res. 1973 Jan;33(1):159-65. |
Description | 5-Azacytidine是DNA甲基转移酶的抑制剂。 | |||||
靶点 | DNA methyltransferase | |||||
IC50 |
质量控制和MSDS
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