Home Epigenetics DNA Methyltransferase inhibitor - Apoptosis related activator - Nucleoside Analog/Antimetabolite inhibitor Decitabine 仅限科研使用

Decitabine

别名: Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716 中文名称：地西他滨

Decitabine是DNA甲基转移酶抑制剂，整合进入DNA、导致DNA低甲基化，并使DNA复制停滞在intra-S-phase。Decitabine被用于治疗骨髓增生异常综合征(MDS)。Decitabine可在多种癌细胞系中诱导细胞周期阻滞和凋亡。

Decitabine Chemical Structure

Decitabine Chemical Structure

CAS: 2353-33-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) 794.43 现货
10mg 647.01 现货
25mg 1203.93 现货
100mg 3030.3 现货
1g 7944.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn
免费分装
免费预溶

Decitabine相关产品

相关信号通路图

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase信号通路图

细胞实验数据示例

细胞系 实验类型 给药浓度 孵育时间 活性描述 文献信息(PMID)
MV4-11 Apoptosis Assay 2.5 μM 48 h  decreases the cell viability co-treated with Tf-NP-sc 23493348
OCI-AML3 Apoptosis Assay 2.5 μM 48 h  decreases the cell viability co-treated with Tf-NP-sc 23493348
Kasumi-1 Apoptosis Assay 0.5 μM 48 h  decreases the cell viability co-treated with Tf-NP-sc 23493348
AGS  Growth Inhibition Assay 5/10/20/50 μM 48 h  induces G2/M phase arrest  23582784
A549 Apoptosis Assay 5/10/20/50 μM 48 h  inhibits the cell viability  23582784
AGS Apoptosis Assay 5/10/20/50 μM 48 h  inhibits the cell viability  23582784
BT‑474 Function Assay 0.2/1 μM 72 h causes re-expression of claudin 1  23844228
HCC1569 Function Assay 0.2/1 μM 72 h causes re-expression of claudin 1  23844228
MDA‑MB‑453 Function Assay 0.2/1 μM 72 h causes re-expression of claudin 1  23844228
HL-60 Growth Inhibition Assay 1 μM 48 h increases G2-phase cell fraction 24000324
U251 Apoptosis Assay 1/10/100 μM 7 d induces cell apoptosis in a dose-dependent manner 24146874
QBC-939 Apoptosis Assay 1/10/100 μM 7 d induces cell apoptosis in a dose-dependent manner 24146874
LS174T Apoptosis Assay 1/10/100 μM 7 d induces cell apoptosis in a dose-dependent manner 24146874
HepG2 Apoptosis Assay 1/10/100 μM 7 d induces cell apoptosis in a dose-dependent manner 24146874
LS174T Function Assay 0.5/1 μM 24 h lead to an increase of OCTN2 levels 24146874
HepG2 Function Assay 0.5/1 μM 24 h up-regulated the relative OCTN2 mRNA and protein expression 24146874
U937-A/E-9/14/18  Apoptosis Assay 0.01/0.1/1/10 μM 48 h induces cell apoptosis in a dose-dependent manner 24300456
HCT-116 Function Assay 250/500nM 48 h do not induces delayed and sustained ROS increase 24423613
DLD-1 Function Assay 250/500nM 48 h do not induces delayed and sustained ROS increase 24423613
ML-1 Function Assay 250/500nM 48 h induces delayed and sustained ROS increase 24423613
HL-60 Function Assay 250/500nM 48 h induces delayed and sustained ROS increase 24423613
CEM Function Assay 250/500nM 48 h induces delayed and sustained ROS increase 24423613
BV-173 Function Assay 250/500nM 48 h induces delayed and sustained ROS increase 24423613
KG-1a Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h induces cell apoptosis in both dose- and time- dependent manner 24423613
HL-60 Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h induces cell apoptosis in both dose- and time- dependent manner 24423613
ML-1 Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h induces cell apoptosis in both dose- and time- dependent manner 24423613
BV-173 Apoptosis Assay 0.25/0.5/0.75/1 μM 48/72/96 h induces cell apoptosis in both dose- and time- dependent manner 24423613
NB4 Function Assay 2.5/5/7.5/10 μM 24 h increasea the expression of precursor miR-125a 24484870
NCI-H929  Growth Inhibition Assay 1/2 μM 24/48/72 h affects cell cycle progression negatively 24833108
JJN3  Growth Inhibition Assay 0.5/1 μM 24/48/72 h affects cell cycle progression negatively 24833108
OPM-2  Growth Inhibition Assay 1/2 μM 24/48/72 h affects cell cycle progression negatively 24833108
RPMI-8226 Growth Inhibition Assay 1/2 μM 24/48/72 h affects cell cycle progression negatively 24833108
NCI-H929  Apoptosis Assay 1/2 μM 72/96/120 h induces cell apoptosis 24833108
JJN3  Apoptosis Assay 0.5/1 μM 24/48 h induces cell apoptosis 24833108
OPM-2  Apoptosis Assay 1/2 μM 72/96/120 h induces cell apoptosis 24833108
RPMI-8226 Apoptosis Assay 1/2 μM 48/72/96 h induces cell apoptosis 24833108
LOVO Apoptosis Assay 10 μM 48 h enhances Gefitinib-induced apoptosis 24874286
SW1116  Apoptosis Assay 10 μM 48 h enhances Gefitinib-induced apoptosis 24874286
LOVO Function Assay 10 μM 48 h increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib 24874286
SW1116  Function Assay 10 μM 48 h increases the effective at inhibiting AKT and mTOR signaling pathways combined with gefitinib 24874286
LOVO Growth Inhibition Assay 0.5/1/2/5 μM 48 h enhances the Gefitinib induced cell inhibition 24874286
SW1116  Growth Inhibition Assay 0.5/1/2/5 μM 48 h enhances the Gefitinib induced cell inhibition 24874286
Eca109 Function Assay 0.5/1 μM 24 h decreases expression of NF-κB2 and MMP2 25123082
Eca109 Growth Inhibition Assay 0.5 μM 24 h induces G2/M arrest in the cell cycle 25123082
Eca109 Function Assay 0.5 μM 24 h inhibits cell invasion 25123082
Eca109 Function Assay 0.5 μM 6/12/24 h inhibits cell migration  25123082
Eca109 Growth Inhibition Assay 0.5/2.5/5 μM 24/48/72 h inhibits cell growth in both dose- and time- dependent manner 25123082
Eca109 Function Assay 0.5 μM 24 h modulates the gene expression of MAGE-A members 25123082
NK  Cytotoxity Assay 0.02-20 μM 5 d decreases the cytolytic activity of NK cells at intermediate concentrations resulting in a U-shaped dose–response curve 23328088
NK  Apoptosis Assay 0.02-20 μM 5 d decrease NK cell proliferation and viability as the concentration increased 23328088
NK  Function Assay 0.01-20 μM 5 d causes hypomethylation of NK cells in a dose–response 23328088
MOLT4/DNR Function Assay 5 μM 4 d reduces ABCB1 mRNA expression 23060570
Jurkat/DOX Function Assay 5 μM 4 d reduces ABCB1 mRNA expression 23060570
MOLT4/DNR Growth Inhibition Assay 5 μM 4 d reduces the IC50 value for daunorubicin sensitivity 23060570
Jurkat/DOX Growth Inhibition Assay 5 μM 4 d reduces the IC50 value for daunorubicin sensitivity 23060570
ccRCC  Apoptosis Assay 0.01-10μM 72 h has minimal effect on cell proliferation 22826467
TNBC  Apoptosis Assay 0.01-10μM 72 h has minimal effect on cell proliferation 22826467
A498 Apoptosis Assay 0.01-10μM 72 h induces synergistic responses with romidepsin 22826467
KIJ265T Apoptosis Assay 0.01-10μM 72 h induces synergistic responses with romidepsin 22826467
MDA-231 Apoptosis Assay 0.01-10μM 72 h induces synergistic responses with romidepsin 22826467
BT-20 Apoptosis Assay 0.01-10μM 72 h induces synergistic responses with romidepsin 22826467
U937 Growth Inhibition Assay 5-20 μM 24/48/72 h induces a decrease in cell viability in a concentration- and time-dependent manner 22767021
HL60 Growth Inhibition Assay 5-20 μM 24/48/72 h induces a decrease in cell viability in a concentration- and time-dependent manner 22767021
U937 Apoptosis Assay 15 μM 24/48/72 h induces cell apoptosis 22767021
HL60 Apoptosis Assay 15 μM 24/48/72 h induces cell apoptosis 22767021
LS411N  Apoptosis Assay 0.5 μM 72 h increases Fas mRNA level 22461695
MDA-MB-231 Apoptosis Assay 10 μM 48 h reduces cell viability in a dose-dependent manner 21887697
MCF-7  Apoptosis Assay 10 μM 48 h reduces cell viability in a dose-dependent manner 21887697
A375 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
SKMEL1 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
SKMEL3 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
SKMEL28 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
MeWo Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
B16 Growth Inhibition Assay 0.5 μM 1/5/8 d inhibits proliferation and induces differentiation of melanoma cells 21796622
U373-MAGI Antiviral assay 0.25 to 8 uM 2 to 72 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in U5-gag level at 0.25 to 8 uM after 2 to 72 hrs by qPCR method 27117260
U373-MAGI Antiviral assay 0.25 to 8 uM 2 to 72 hrs Antiviral activity against VSV-G pseudotyped HIV-1 NL4-3 infected in human U373-MAGI cells assessed as reduction in gag level at 0.25 to 8 uM after 2 to 72 hrs by qPCR method 27117260
CD4+ CD25− T  Function Assay 1/5 μM reduceS global DNA methylation 24476360
HCT116 Growth Inhibition Assay 72 h IC50=1.7±0.4 μM 24172061
SW48 Growth Inhibition Assay 72 h IC50=15.2±6.2 μM 24172061
HT29 Growth Inhibition Assay 72 h IC50=1400±179 μM 24172061
Ly 1 Growth Inhibition Assay 24 h IC50=7.3 μM 21772049
Ly 7 Growth Inhibition Assay 24 h IC50=10.7 μM 21772049
Su-DHL6 Growth Inhibition Assay 24 h IC50＞20 μM 21772049
Ly 10 Growth Inhibition Assay 24 h IC50＞20 μM 21772049
RIVA Growth Inhibition Assay 24 h IC50＞20 μM 21772049
Su-DHL2 Growth Inhibition Assay 24 h IC50＞20 μM 21772049
Ly 1 Growth Inhibition Assay 48 h IC50=0.34 μM 21772049
Ly 7 Growth Inhibition Assay 48 h IC50=0.025 μM 21772049
Su-DHL6 Growth Inhibition Assay 48 h IC50＞20 μM 21772049
Ly 10 Growth Inhibition Assay 48 h IC50=1.8 μM 21772049
RIVA Growth Inhibition Assay 48 h IC50＞20 μM 21772049
Su-DHL2 Growth Inhibition Assay 48 h IC50=17.4 μM 21772049
Ly 1 Growth Inhibition Assay 72 h IC50=0.01 μM 21772049
Ly 7 Growth Inhibition Assay 72 h IC50=0.018 μM 21772049
Su-DHL6 Growth Inhibition Assay 72 h IC50=1.6 μM 21772049
Ly 10 Growth Inhibition Assay 72 h IC50=1.2 μM 21772049
RIVA Growth Inhibition Assay 72 h IC50＞20 μM 21772049
Su-DHL2 Growth Inhibition Assay 72 h IC50=11.2 μM 21772049
HeLa Kinase Assay Ki=14.4 ± 4.6 μM for hCNT3 24780098
HeLa Kinase Assay Ki=21.6 ± 3.0 μM for hCNT1 24780098
HeLa Kinase Assay Ki=5.6 ± 0.5 μM for hENT2 24780098
HeLa Kinase Assay Ki=1000–5000 μM for hENT1 24780098
点击查看更多细胞系数据

生物活性

产品描述 Decitabine是DNA甲基转移酶抑制剂，整合进入DNA、导致DNA低甲基化，并使DNA复制停滞在intra-S-phase。Decitabine被用于治疗骨髓增生异常综合征(MDS)。Decitabine可在多种癌细胞系中诱导细胞周期阻滞和凋亡。
特性 Decitabine 是DNA甲基化的有效抑制剂。
靶点
DNA methylation [1]
(HL-60, KG1a cells)
体外研究(In Vitro)
体外研究活性

Decitabine 有效抑制DNA 合成，这种作用存在剂量依赖性，作用于HL-60和 KG1a 白血病细胞时，IC50分别为 100 ng/mL 和1 ng/mL。Decitabine 抑制细胞生长，这种作用存在剂量和时间依赖性，处理HL-60和KG1a白血病细胞72小时和96小时，IC50分别约为100 ng/mL 和 10 ng/mL。[1] 最新研究显示Decitabine作用于间变性大细胞淋巴瘤(ALCL)，具有抗增殖和促凋亡活性，且抑制KARPAS-299细胞中[3H]胸甘的摄取，EC50 为0.49 μM。[2]
激酶实验 DNA合成检测
通过测定放射性胸甘摄入到DNA的情况而测定DNA合成比率。HL-60 和KG1a 细胞悬浮在6孔(直径为35 mm )盘中，孔中为含10%胎牛血清的2 mL RPMI 培养基中,然后与不同浓度相应药物温育48小时 (药物同时加入)。48小时时, 每孔加入0.5 μCi [3H] 胸甘(6.7 Ci/mmol)，再温育24小时。细胞置于GF/C玻璃纤维过滤器(直径为2.4 cm)中，使用冷 0.9% NaCl, 5% 冷三氯乙酸和乙醇清洗。烘干含DNA的过滤器，置于EcoLite闪烁液(ICN)中，使用 Beckman LS 6000IC 闪烁计数器测量放射性。通过剂量-反应曲线计算IC50值。
细胞实验 细胞系 HL-60 和 KG1a
浓度 0 到100 ng/mL
孵育时间 96 小时
方法

生长抑制实验中，指数生长期细胞接种在5 ml培养基中。向培养基中同时加入不同浓度Decitabine。在指定时间，使用模型 ZM Coulter 计数器对细胞进行计数。根据药物处理的白血病细胞的生长曲线，测定IC50值。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot Survivin / Bcl-2 / p53 / c-Myc / DNMT1 p-AKT / AKT / p-GSK3β / GSK3β / p-Myc / Myc / p-P70 / P70 / p-4EBP-1 / 4EBP-1 / PTEN phospho-p38 / p38 / phospho-NFκB / NFκB p-JAK1 / JAK1 / p-JAK2 / JAK2 / p-STAT3 / STAT3 E-cadherin / N-cadherin / Snail / MMP-2 / MMP-9 / Bcl-2 / Bax 26384351
Immunofluorescence DNMT1 E-cadherin / MMP-9 21303982
Growth inhibition assay Cell viability 26384351
体内研究(In Vivo)
体内研究活性

Decitabine 按2.5 mg/kg 剂量作用于ALK+ KARPAS-299小鼠移植瘤模型，促进凋亡，且降低肿瘤细胞增殖，也导致肿瘤抑制基因p16INK4A的去甲基化。 [2]
动物实验 Animal Models KARPAS-299 人类细胞皮下接种到小鼠的左右两侧。
Dosages ≤2.5 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06291285 Not yet recruiting
Healthy Volunteers
Novo Nordisk A/S
 February 27 2024 Phase 1
NCT05960773 Recruiting
Mesothelioma|Malignant Mesothelioma (MM)|Early-stage Mesothelioma|Subclinical Mesothelioma|BRCA1-Associated Protein-1 (BAP1) Mutations|Early-stage BAP1-associated Malignancies
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
 January 31 2024 Phase 2
NCT05835011 Terminated
Myelodysplastic Syndromes
Astex Pharmaceuticals Inc.
 July 14 2023 Phase 2
NCT05816356 Recruiting
Healthy
EpiDestiny Inc.|Worldwide Clinical Trials
 March 24 2023 Phase 1
  • https://pubmed.ncbi.nlm.nih.gov/12620295/
  • https://pubmed.ncbi.nlm.nih.gov/22687603/

化学信息&溶解度

分子量 228.21 分子式

C8H12N4O4
CAS号 2353-33-5 SDF Download Decitabine SDF
Smiles C1C(C(OC1N2C=NC(=NC2=O)N)CO)O
储存条件(自收到货起)

体外溶解度
批次：

DMSO : 45 mg/mL ( (197.18 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : 22.5 mg/mL (98.59 mM)

Ethanol : Insoluble

摩尔浓度计算器

体内溶解配方
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

 动物体内配方计算器

实验计算

摩尔浓度计算器

质量 浓度 体积 分子量

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

mg/kg g μL 只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

* 必填项

请输入您的姓名
请输入您的邮箱地址 请输入一个有效的邮箱地址
请写点东西给我们

常见问题及建议解决方法

问题 1:
Is S1200 a racemic mixture or a monomer?

回答：
S1200 is R form

在线咨询
联系我们