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

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。

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

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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。

Decitabine/地西他宾 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/地西他宾 细胞实验

Cell Line
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.

Decitabine/地西他宾 动物实验

Species
Animal Model
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.

Decitabine/地西他宾 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
V 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/地西他宾 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/地西他宾 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/地西他宾 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/地西他宾 技术信息

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

请根据您的动物给药指南选择适当的溶解方案。
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
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 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
方案 一
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