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Decitabine

別名: Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716 中文名稱：地西他濱

Decitabine是DNA甲基轉(zhuǎn)移酶抑制劑，整合進入DNA、導(dǎo)致DNA低甲基化，并使DNA復(fù)制停滯在intra-S-phase。Decitabine被用于治療骨髓增生異常綜合征(MDS)。Decitabine可在多種癌細胞系中誘導(dǎo)細胞周期阻滯和凋亡。

Decitabine Chemical Structure

Decitabine Chemical Structure

CAS: 2353-33-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 794.43 現(xiàn)貨
10mg 647.01 現(xiàn)貨
25mg 1203.93 現(xiàn)貨
100mg 3030.3 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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Decitabine相關(guān)產(chǎn)品

相關(guān)信號通路圖

DNA Methyltransferase Signaling Pathways

DNA Methyltransferase信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
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
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生物活性

產(chǎn)品描述 Decitabine是DNA甲基轉(zhuǎn)移酶抑制劑，整合進入DNA、導(dǎo)致DNA低甲基化，并使DNA復(fù)制停滯在intra-S-phase。Decitabine被用于治療骨髓增生異常綜合征(MDS)。Decitabine可在多種癌細胞系中誘導(dǎo)細胞周期阻滯和凋亡。
特性 Decitabine 是DNA甲基化的有效抑制劑。
靶點
DNA methylation [1]
(HL-60, KG1a cells)
體外研究(In Vitro)
體外研究活性

Decitabine 有效抑制DNA 合成，這種作用存在劑量依賴性，作用于HL-60和 KG1a 白血病細胞時，IC50分別為 100 ng/mL 和1 ng/mL。Decitabine 抑制細胞生長，這種作用存在劑量和時間依賴性，處理HL-60和KG1a白血病細胞72小時和96小時，IC50分別約為100 ng/mL 和 10 ng/mL。[1] 最新研究顯示Decitabine作用于間變性大細胞淋巴瘤(ALCL)，具有抗增殖和促凋亡活性，且抑制KARPAS-299細胞中[3H]胸甘的攝取，EC50 為0.49 μM。[2]
激酶實驗 DNA合成檢測
通過測定放射性胸甘攝入到DNA的情況而測定DNA合成比率。HL-60 和KG1a 細胞懸浮在6孔(直徑為35 mm )盤中，孔中為含10%胎牛血清的2 mL RPMI 培養(yǎng)基中,然后與不同濃度相應(yīng)藥物溫育48小時 (藥物同時加入)。48小時時, 每孔加入0.5 μCi [3H] 胸甘(6.7 Ci/mmol)，再溫育24小時。細胞置于GF/C玻璃纖維過濾器(直徑為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的過濾器，置于EcoLite閃爍液(ICN)中，使用 Beckman LS 6000IC 閃爍計數(shù)器測量放射性。通過劑量-反應(yīng)曲線計算IC50值。
細胞實驗 細胞系 HL-60 和 KG1a
濃度 0 到100 ng/mL
孵育時間 96 小時
方法

生長抑制實驗中，指數(shù)生長期細胞接種在5 ml培養(yǎng)基中。向培養(yǎng)基中同時加入不同濃度Decitabine。在指定時間，使用模型 ZM Coulter 計數(shù)器對細胞進行計數(shù)。根據(jù)藥物處理的白血病細胞的生長曲線，測定IC50值。
實驗圖片 檢測方法 檢測指標 實驗圖片 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 28152502
Immunofluorescence E-cadherin / MMP-9 DNMT1 28152502
Growth inhibition assay Cell viability 26384351
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Decitabine 按2.5 mg/kg 劑量作用于ALK+ KARPAS-299小鼠移植瘤模型，促進凋亡，且降低腫瘤細胞增殖，也導(dǎo)致腫瘤抑制基因p16INK4A的去甲基化。 [2]
動物實驗 Animal Models KARPAS-299 人類細胞皮下接種到小鼠的左右兩側(cè)。
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

化學(xué)信息&溶解度

分子量 228.21 分子式

C8H12N4O4
CAS號 2353-33-5 SDF Download Decitabine SDF
Smiles C1C(C(OC1N2C=NC(=NC2=O)N)CO)O
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 45 mg/mL ( (197.18 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 22.5 mg/mL (98.59 mM)

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

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

回答：
S1200 is R form

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