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
CAS: 2353-33-5
产品质控
批次：
纯度：
99.90%
99.90
Decitabine相关产品
| 相关靶点 | TET DNMT1 DNMT3 | 点击展开 |
|---|---|---|
| 相关产品 | RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol Bobcat339 hydrochloride CM272 GSK3685032 β-thujaplicin | 点击展开 |
| 相关化合物库 | 激酶抑制剂库 FDA药物库 天然产物库 已知活性药物库-I 生物活性库Ⅱ | 点击展开 |
相关信号通路图
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 |
|---|---|---|---|---|---|
| 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 |
|
| 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] |
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|---|---|---|---|---|
| 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。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | E-cadherin / N-cadherin / Snail / MMP-2 / MMP-9 / Bcl-2 / Bax p-JAK1 / JAK1 / p-JAK2 / JAK2 / p-STAT3 / STAT3 phospho-p38 / p38 / phospho-NFκB / NFκB p-AKT / AKT / p-GSK3β / GSK3β / p-Myc / Myc / p-P70 / P70 / p-4EBP-1 / 4EBP-1 / PTEN Survivin / Bcl-2 / p53 / c-Myc / DNMT1 |
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28152502 | |
| Immunofluorescence | E-cadherin / MMP-9 DNMT1 |
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28152502 | |
| Growth inhibition assay | Cell viability |
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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] |
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|---|---|---|
| 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 |
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) | |||
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体外溶解度 |
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 |
|
体内溶解度 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
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。
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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
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