货号:A156645
同义名:
地西他滨
/ 5-Aza-2'-deoxycytidine; 5AZA
Decitabine是一种强效的 DNA 甲基转移酶抑制剂,其在 HL-60 和 KG1a 细胞中的 IC50 值分别为 438 nM 和 4.38 nM。


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| 产品名称 | DNA Methyltransferase ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 6-Thioguanine | ✔ | 98% | |||||||||||||||||
| Zebularine | ✔ | 98% | |||||||||||||||||
| Procainamide HCl | ✔ | 99% | |||||||||||||||||
| 5-Azacytidine | ✔ | 95% | |||||||||||||||||
| Decitabine | ✔ | 99% | |||||||||||||||||
| SGI-1027 |
++
DNMT3A, IC50: 7.5 μM DNMT1, IC50: 6 μM |
99%+ | |||||||||||||||||
| RG108 |
+++
DNA methyltransferase, IC50: 115 nM |
99%+ | |||||||||||||||||
| Guadecitabine sodium | ✔ | 98% | |||||||||||||||||
| 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。 | |||||||||||||||||||
| 靶点 |
|
| 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]. |
| Concentration | Treated Time | Description | References | |
| MOLM13 cells | 100 nM | 72 hours | Assessed proliferation and metabolic activity, DEC significantly reduced cell counts and metabolism | Mol Oncol. 2025 May;19(5):1404-1421 |
| MV4;11 cells | 100 nM | 72 hours | Assessed proliferation and metabolic activity, DEC significantly reduced cell counts and metabolism | Mol Oncol. 2025 May;19(5):1404-1421 |
| NALM-6 cells | 100 nM | 72 hours | Assessed proliferation and metabolic activity, DEC significantly reduced cell counts and metabolism | Mol Oncol. 2025 May;19(5):1404-1421 |
| REH cells | 100 nM | 72 hours | Assessed proliferation and metabolic activity, DEC significantly reduced cell counts and metabolism | Mol Oncol. 2025 May;19(5):1404-1421 |
| RS4;11 cells | 100 nM | 72 hours | Assessed proliferation and metabolic activity, DEC had minimal effect on cell counts and metabolism | Mol Oncol. 2025 May;19(5):1404-1421 |
| SEM cells | 100 nM | 72 hours | Assessed proliferation and metabolic activity, DEC significantly reduced cell counts and metabolism | Mol Oncol. 2025 May;19(5):1404-1421 |
| SW620 cells | 2.5 μM and 5 μM | 72 hours | To investigate the activation of PEPT1 transcription by DAC, results showed DAC activated PEPT1 transcription in a dose-dependent manner. | Cell Death Dis. 2021 May 24;12(6):532. |
| SW480 cells | 2.5 μM and 5 μM | 72 hours | To investigate the activation of PEPT1 transcription by DAC, results showed DAC activated PEPT1 transcription in a dose-dependent manner. | Cell Death Dis. 2021 May 24;12(6):532. |
| MTT cells | 10^-4 mol/L VPA and 10^-7 mol/L DAC | 2 days | Investigate the effects of VPA and DAC on SSTR2 levels and radioligand uptake in MTT cells. Results showed that the combination of VPA and DAC significantly increased SSTR2 levels and radioligand uptake. | Theranostics. 2023 Jan 1;13(1):278-294. |
| MPC cells | 10^-4 mol/L VPA and 10^-7 mol/L DAC | 2 days | Investigate the effects of VPA and DAC on SSTR2 levels and radioligand uptake in MPC cells. Results showed that DAC alone or in combination with VPA increased SSTR2 levels and radioligand uptake. | Theranostics. 2023 Jan 1;13(1):278-294. |
| Human umbilical vein endothelial cells (HUVECs) | 10 μmol/L | 24 hours | Inhibition of DNMTs suppressed the disturbed flow/OS-induced EndoMT and ameliorated the downregulation of ALDHs and β-alanine biosynthesis. | Theranostics. 2023 Aug 6;13(13):4392-4411 |
| HCT116 cells | 2.5 μM | 24–72 h | Inhibited methylation and increased HOXB13 expression | Signal Transduct Target Ther. 2019 Nov 29;4:51. |
| RKO cells | 2.5 μM | 24–72 h | Inhibited methylation and increased HOXB13 expression | Signal Transduct Target Ther. 2019 Nov 29;4:51. |
| Alb-R26Met HCC cells | 0.3 µM | 48 h | Decitabine treatment does not affect the viability of Alb-R26Met HCC cells but interferes with their tumorigenic properties, as evidenced by reduced colony numbers in anchorage-independent growth, reduced number and size of foci in anchorage-dependent growth, and reduced tumor spheres in self-renewal conditions. | Nat Commun. 2018 Aug 8;9(1):3164. |
| T-ALL cells | 1 μM | 48 h | To evaluate the effect of Decitabine on T-ALL cell lines, results showed that Decitabine significantly upregulated tumor suppressor genes (e.g., BMF and BBC3) and downregulated the MYC pathway. | Blood Cancer Discov. 2020 Nov;1(3):274-289. |
| HGC27 cells | 20μM | 72 h | Decitabine synergized with COX inhibitors to reduce cell viability in HGC27 cells | Theranostics. 2019 Aug 14;9(21):6256-6268. |
| MKN1 cells | 20μM | 72 h | Decitabine synergized with COX inhibitors to reduce cell viability in MKN1 cells | Theranostics. 2019 Aug 14;9(21):6256-6268. |
| PUER cells | 0.5 µM | Decitabine addition concurrent with OHT attenuated the repression of stem cell genes and the activation of differentiation genes, thereby maintaining self-renewal of hematopoietic precursors | Mol Cancer Ther. 2010 Jun;9(6):1536-43. | |
| Human CD34+ hematopoietic precursors | 0.5 µM | Decitabine addition concurrent with G-CSF attenuated the repression of stem cell genes and the activation of differentiation genes, thereby maintaining self-renewal of hematopoietic precursors | Mol Cancer Ther. 2010 Jun;9(6):1536-43. | |
| ML-2 cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| K562 cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| U937 cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| HL-60 cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| KG-1 cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| KG-1a cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| HCT116 cells | 100 nM | 24 h | Quantitative determination of Decitabine incorporation into DNA, showing significant incorporation of Decitabine | Nucleic Acids Res. 2014 Oct 29;42(19):e152. |
| Administration | Dosage | Frequency | Description | References | ||
| Mice | SEM-fluc and RS4;11-fluc cell line-derived xenograft models | Intraperitoneal injection | 0.4 mg/kg | 4 consecutive days starting 7 days after tumor cell injection | Assessed the effect of DEC on tumor cell proliferation, DEC significantly delayed tumor cell proliferation | Mol Oncol. 2025 May;19(5):1404-1421 |
| Mice | MC38 tumor model | Intraperitoneal injection | 0.2 mg/kg/day | 5 consecutive days | DAC combined with anti-PD-1 significantly inhibited tumor growth, promoted TILs infiltration, and enhanced CD8+ T cell function | Mol Cancer. 2023 May 16;22(1):84 |
| Mice | Endothelial lineage tracing mice and conditional EC Dnmt1 knockout mice | Intraperitoneal injection | 0.2 mg/kg | 6 consecutive days of injection and 1 day of rest as intervals for 3 weeks | Endothelial-specific knockout of Dnmt1 protected the vasculature from disturbed flow-induced remodeling and atherosclerosis. | Theranostics. 2023 Aug 6;13(13):4392-4411 |
| CD-1 mice | Not specified | Oral gavage | 0.4 mg/kg and 1.0 mg/kg | Single dose | To measure plasma drug levels of Decitabine, results showed significantly lower drug levels in male mice compared to females | Clin Cancer Res. 2013 Feb 15;19(4):938-48 |
| Nude mice | Alb-R26Met HCC cell xenograft model | Intraperitoneal injection | 2.5 mg/kg | Twice a week for three weeks | Decitabine treatment significantly reduced the tumor volume of Alb-R26Met HCC cells in nude mice, and the dose was not toxic. | Nat Commun. 2018 Aug 8;9(1):3164. |
| Mice | T-ALL patient-derived xenograft (PDX) models | Not specified | 0.5 mg/kg | Once daily for 5 days, followed by 2 days off, for two cycles | To evaluate the effect of Decitabine on T-ALL xenograft models, results showed that Decitabine significantly prolonged leukemia-free survival and downregulated the MYC pathway. | Blood Cancer Discov. 2020 Nov;1(3):274-289. |
| Nude mice | HGC27 xenograft model | Intraperitoneal injection | 5mg/kg | 3 times per week for 21 days | Decitabine synergized with Celecoxib to inhibit HGC27 xenograft tumor growth | Theranostics. 2019 Aug 14;9(21):6256-6268. |
| 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 |
|
| 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 << |
| 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 |
|
| CAS号 | 2353-33-5 |
| 分子式 | C8H12N4O4 |
| 分子量 | 228.21 |
| SMILES Code | OC[C@@H]1[C@H](C[C@H](N2C(N=C(N=C2)N)=O)O1)O |
| MDL No. | MFCD00043011 |
| 别名 | 地西他滨 ;5-Aza-2'-deoxycytidine; 5AZA; 5-aza-dCyd; DAC; NSC 127716 |
| 运输 | 蓝冰 |
| InChI Key | XAUDJQYHKZQPEU-KVQBGUIXSA-N |
| Pubchem ID | 451668 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Keep in dark place, inert atmosphere, store in freezer, under -20°C |
| 溶解方案 |
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 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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