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/ Decitabine

地西他宾 /Decitabine {[allProObj[0].p_purity_real_show]}

货号：A156645 同义名： 地西他滨 / 5-Aza-2'-deoxycytidine;5-AZA-CdR

Decitabine is a potent inhibitor of DNA methyltransferase with IC50 of 438 nM and 4.38 nM in HL-60 and KG1a cells, respectively.

Decitabine 化学结构 CAS号：2353-33-5
Decitabine 化学结构
CAS号：2353-33-5
Decitabine 3D分子结构
CAS号：2353-33-5
Decitabine 化学结构 CAS号：2353-33-5
Decitabine 3D分子结构 CAS号：2353-33-5
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Decitabine 纯度/质量文件 产品仅供科研

货号：A156645 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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产品名称 DNA Methyltransferase ↓ 其他靶点 纯度
6-Thioguanine ✔ 98%
Zebularine ✔ 98%
Procainamide hydrochloride ✔ 99%
5-Azacytidine ✔ 95%
Decitabine ✔ 99%
SGI-1027 ++

DNMT1, IC50: 6 μM

DNMT3A, IC50: 7.5 μM

 		99%+
RG108 +++

DNA methyltransferase, IC50: 115 nM

 		99%+
Guadecitabine sodium ✔ 99+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Decitabine 生物活性

靶点

  • DNA Methyltransferase
描述 The DNA methyltransferase (DNMT) family are enzymes that can mediate the DNA methylation. Inhibiting the DNMTs have shown particular promise in reducing the formation of tumors[5]. The decitabine is a potent inhibitor of the DNA methylation with IC50 value of 100 and 10 ng/ml for 72 and 96h of exposure on both HL-60 and KG1a leukemic cells[6]. The human aortic smooth muscle cells (HASMCs) were treated with decitabine for 48 hours. The DNMT1 expression measured by western blotting assay in the nuclear fraction was reduced by the decitabine. The expression of the osteogenic genes ALP, Max2, BMP2, Pit-1, SM22 and -SMA in HASMCs measured by RT-qPCR was increased by decitabine[7]. The hyperoxia-indued lung injury Sprague-Dawley rats were injected with decitabine at a dose of 0.5 mg/kg/day for 14 days. The survival rate of the treatment group was significantly higher than the hyperoxia group. The P16 methylation rate in the lung tissues measured by PCR was induced by the hyperoxia and the decitabine could effectively reverse the hypermethylation of P16[8].
作用机制 Decitabine could combine with DNA during DNA replication and form covalent complexes with the DNMT1. Therefore, the methyl transfer activity of the enzyme is inhibited[8].

Decitabine 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 数据源
A375 0.5 μM Growth Inhibition Assay 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
A498 0.01-10μM Apoptosis Assay 72 h induces synergistic responses with romidepsin 22826467
A549 5/10/20/50 μM Apoptosis Assay 48 h  inhibits the cell viability  23582784
AGS 5/10/20/50 μM Apoptosis Assay 48 h  inhibits the cell viability  23582784

Decitabine 动物研究

Dose Mice: 50 mg/kg - 150 mg/kg[3] (i.v.), 1 mg/kg - 32 mg/kg[3] (i.p.), 25 mg/kg[4] (p.o.)
Administration i.v., i.p., p.o.
Pharmacokinetics
Animal Dogs[4]
Dose 4 mg/kg
Administration i.v.
t1/2β 69 ± 4.5 min
t1/2α 5.5 ± 0.9 min
Vdβ 958 ± 164 ml/kg
CL 6.6 ± 0.9 ml/min/kg
Vdss 779 ± 102 ml/kg
AUC0→∞ 478 ± 54 μg/ml/min
K10 0.021 ± 0.004 min-1

Decitabine 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02564536 Chronic Myelomonocytic Leukemi... 展开 >>a Juvenile Myelomonocytic Leukemia Atypical Chronic Myeloid Leukemia Myeloproliferative Neoplasm Myelodysplastic Syndromes Myelofibrosis 收起 << Phase 1 Withdrawn(Lack of funding foll... 展开 >>owing full FDA clinical hold) 收起 << June 30, 2020 -
NCT01130506 Previously Treated Myelodyspla... 展开 >>stic Syndrome Recurrent Adult Acute Myeloid Leukemia Refractory Acute Myeloid Leukemia Secondary Acute Myeloid Leukemia Therapy-Related Acute Myeloid Leukemia Untreated Adult Acute Myeloid Leukemia 收起 << Phase 1 Completed - United States, Ohio ... 展开 >> Ohio State University Comprehensive Cancer Center Columbus, Ohio, United States, 43210 United States, Texas M D Anderson Cancer Center Houston, Texas, United States, 77030 收起 <<
NCT03240211 PTCL CTCL Phase 1 Recruiting December 2020 United States, New York ... 展开 >> 51 West 51st Street, Suite 200 Recruiting New York, New York, United States, 10019 Contact: Michelle Malanga    212-326-5731    mm4629@cumc.columbia.edu    Italy University of Bologna Not yet recruiting Bologna, Italy Principal Investigator: Pier Luigi Zinzani, MD, PhD          Korea, Republic of Samsung Medical Center Not yet recruiting Seoul, Korea, Republic of Principal Investigator: Won Seog Kim, MD, PhD 收起 <<

Decitabine 参考文献

[1]Decitabine

[2]Decitabine

[3]9:305.

[4]27(5):437-44.

[5]Gravina GL, Festuccia C, Marampon F, Popov VM, Pestell RG, Zani BM, Tombolini V. Biological rationale for the use of DNA methyltransferase inhibitors as new strategy for modulation of tumor response to chemotherapy and radiation. Mol Cancer. 2010 Nov 25;9:305.

[6]Shaker S, Bernstein M, Momparler LF, Momparler RL. Preclinical evaluation of antineoplastic activity of inhibitors of DNA methylation (5-aza-2'-deoxycytidine) and histone deacetylation (trichostatin A, depsipeptide) in combination against myeloid leukemic cells. Leuk Res. 2003 May;27(5):437-44.

Decitabine 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.38mL

0.88mL

0.44mL

21.91mL

4.38mL

2.19mL

43.82mL

8.76mL

4.38mL

Decitabine 技术信息

CAS号2353-33-5
分子式C8H12N4O4
分子量 228.205
别名 地西他滨 ;5-Aza-2'-deoxycytidine;5-AZA-CdR;US brand name: Dacogen. Abbreviations: 5AZA;dezocitidine;deoxyazacytidine;5-aza-dCyd;5-aza-2’-Deoxycytidine;DAC;NSC 127716
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
溶解度

DMSO: 50 mg/mL(219.1 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 20 mg/mL(87.64 mM)，配合低频超声助溶
动物实验配方

Tags: Decitabine | 5-Aza-2'-deoxycytidine;5-AZA-CdR; Abbreviations: 5AZA;dezocitidine;deoxyazacytidine;5-aza-dCyd;5-aza-2’-Deoxycytidine;DAC;NSC 127716 | 地西他滨 | Antivirus | DNA Methyltransferase | AmBeed-信号通路专用抑制剂 | Decitabine 纯度/质量文件 | Decitabine 亚型比较 | Decitabine 生物活性 | Decitabine 细胞研究 | Decitabine 动物研究 | Decitabine 临床数据 | Decitabine 参考文献 | Decitabine 实验方案 | Decitabine 技术信息

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