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My CartCAS：2353-33-5
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：HPLC≥98%
Appearance：White to off-white Solid
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| CAS | 2353-33-5 |
| Name | Decitabine |
| Molecular Formula | C8H12N4O4 |
| Molecular Weight | 228.21 |
| Solubility | Soluble in DMSO |
| Purity | HPLC≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC | EINECS 219-089-4 |
| MDL | MFCD00043011 |
| SMILES | O=C1N=C(N)N=CN1[C@H](O[C@@H]2CO)C[C@@H]2O |
| InChIKey | XAUDJQYHKZQPEU-KVQBGUIXSA-N |
| InChI | InChI=1S/C8H12N4O4/c9-7-10-3-12(8(15)11-7)6-1-4(14)5(2-13)16-6/h3-6,13-14H,1-2H2,(H2,9,11,15)/t4-,5+,6+/m0/s1 |
| PubChem CID | 451668 |
| Target Point | DNA Methyltransferase |
| Passage | Epigenetics |
| Background | Decitabine is an orally active DNA methyltransferase inhibitor. Incorporation of Decitabine instead of DNA into cytosine can covalently capture DNA methyltransferase into DNA， resulting in irreversible inhibition of the enzyme. Decitabine induces cell G2/M block and apoptosis， and has effective anticancer activity. |
| Biological Activity | Decitabine (NSC 127716) 是一种DNA甲基转移酶抑制剂，通常用于治疗骨髓增生异常综合征(MDS) 和急性髓性白血病 (AML)。[1-5] |
| In Vitro | 地西他滨处理在接触地西他滨后96小时显著抑制SNU719，NCC24和KATOIII的细胞生长。地西他滨诱导EBVaGC中G2/M阻滞和凋亡，抑制侵袭能力，并上调EBVaGC的E-钙粘蛋白表达[1]。在MDS-L敏感细胞中进行DAC处理后，H4N末端尾部(H4K8acK12acK16ac)的三乙酰化降低[2]。地西他滨上调HeLa细胞中的DCTPP1和dUTPase表达[3]。 |
| In Vivo | 地西他滨(1.0 mg/kg，po)与四氢尿苷(THU)联合使用会导致女性出现严重毒性，导致对地西他滨毒性的敏感性增加与地西他滨血浆水平相关[4]。 |
| Cell Experiment | 通过细胞计数和MTS测定分析细胞活力。将SNU719，NCC24和KATOIII以5×10 4个细胞/ mL的密度接种，仅与补充有FBS的RPMI-1640一起培养24小时。温育24小时后，在存在或不存在地西他滨(DAC)的情况下处理细胞120小时。用于细胞计数的细胞用胰蛋白酶消化并在DAC处理后0，24，48，72，96和120小时计数。通过台盼蓝排除法确定活细胞。对于MTS测定，将细胞(SNU719和NCC24：1×10 4 /孔，KATOIII：1×10 3 /孔)接种到96孔培养皿上。接种后，在指定的时间段将MTS加入井中。温育1小时后，在490nm处测量吸光度。 |
| Animal Experiment | 将小鼠分配至四个剂量组和媒介物对照组。在给予四氢尿嘧啶(THU)或其载体以10mL/kg的剂量体积后1小时±5分钟给动物服用地西他滨(DAC)或其载体。基于范围发现研究选择DAC剂量，其中小鼠耐受六个口服剂量(2x /周)的0.1，0.2和0.4mg/kg DAC以及固定剂量的167mg/kg THU。选择固定的THU剂量(500mg/m 2)和THU与DAC给药之间的最佳时间(60分钟)。将小鼠中每体表面积剂量的毫克转换成毫克每千克体重剂量估计基于小鼠的米氏常数(Km)值。简而言之，小鼠剂量(毫克/体表面积(500mg/m 2)除以Km为3，将剂量转换为毫克每千克体重(167mg/kg)。 |
| Kinase Experiment | 使用连续分光光度测定法测定DCTPP1的焦磷酸水解酶活性。在标准反应(1mL最终体积)中，将10-250μM核苷酸底物在反应缓冲液(20mM MgCl 2，100mM KCl，0.75mg/mL BSA和4mM DTT)中孵育，浓度范围为0.1-1。 μM的DCTTP1。所有反应均在25℃下进行。 |
| Data Literature Source | 1]. Nakamura M，et al. Decitabine inhibits tumor cell proliferation and up-regulates E-cadherin expression in Epstein-Barr virus-associated gastric cancer. J Med Virol. 2016 Jul 19. [2]. Zhang C，et al. Quantitative proteomic analysis of histone modifications in decitabine sensitive and resistant leukemia cell lines. Clin Proteomics. 2016 Jul 5;13:14. [3]. Requena CE，et al. The nucleotidohydrolases DCTPP1 and dUTPase are involved in the cellular response to decitabine. Biochem J. 2016 Jun 20. [4]. Terse P，et al. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice. Int J Toxicol. 2014 Mar-Apr;33(2):75-85. [5]. Yu J，et al. DNA methyltransferase expression in triple-negative breast cancer predicts sensitivity to decitabine. J Clin Invest. 2018 Jun 1;128(6):2376-2388. |
| Unit | Bottle |
| Specification | 10mg 10mM*1mL in DMSO 50mg |
是一种DNA甲基转移酶抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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