Decitabine

別名:Deoxycytidine, 5-aza-2'-deoxycytidine, 5-AZA-dC, 5-aza-CdR,NSC 127716

Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.

Decitabine化学構造

CAS No. 2353-33-5

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 29500 国内在庫あり
JPY 22000 国内在庫あり
JPY 38500 国内在庫あり
JPY 56500 国内在庫あり
JPY 86500 国内在庫あり
JPY 220500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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文献中Selleckの製品使用例(180)

製品安全説明書

現在のバッチを見る: 純度: 99.90%
99.90

Decitabine関連製品

DNA Methyltransferase阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 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
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生物活性

製品説明 Decitabine is a DNA methyltransferase inhibitor, incorporating into DNA and resulting in hypomethylation of DNA and intra-S-phase arrest of DNA replication. It is used to treat myelodysplastic syndrome (MDS). Decitabine induces cell cycle arrest and apoptosis in various cancer cell lines.
Targets
DNA methylation [1]
(HL-60, KG1a cells)
In Vitro
In vitro

Decitabine inhibits cell growth in a dose and time-dependent manner with IC50 of approximately 438 nM and 43.8 nM for 72 hours and 96 hours exposure in HL-60 and KG1a leukemic cells, respectively. [1] A recent study shows that Decitabine exhibits high anti-proliferative and pro-apoptotic activity against anaplastic large cell lymphoma (ALCL), and inhibits [3H]–thymidine uptake in KARPAS-299 cells with EC50 of 0.49 μM. [2]

Kinase Assay DNA synthesis assay
The rate of DNA synthesis is measured by the incorporation of radioactive thymidine into DNA. HL-60 and KG1a cells are suspended in 2 mL RPMI medium containing 10% fetal serum in 6-well (35 mm diameter) dishes and incubated with different concentrations of corresponding drugs for 48 hours (drugs are added simultaneously). At 48 hours, 0.5 μCi [3H] thymidine (6.7 Ci/mmol) is added to each well and incubated for an additional 24 hours. The cells are placed on GF/C glass fiber filters (2.4 cm diameter), washed with cold 0.9% NaCl, 5% cold trichloroacetic acid and ethanol. The filters containing the DNA are then dried, placed in EcoLite scintillation liquid (ICN) and the radioactivity measured using Beckman LS 6000IC scintillation counter. The IC50 is defined as the concentration of drug that inhibits 50% of the DNA synthesis of the leukemic cell lines from the dose–response curve.
細胞実験 細胞株 HL-60 and KG1a
濃度 0-500 nM
反応時間 96 hours
実験の流れ

For the growth inhibition assay, cells in log phase are placed in 5 mL of medium. Different concentrations of Decitabine are added to the medium simultaneously. Cell counts are performed at the indicated times using a model ZM Coulter Counter. The concentration that produces 50% inhibition of growth (IC50) is determined from the growth curves of the drug treated leukemic cell lines.

実験結果図 Methods Biomarkers 結果図 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
In Vivo
In Vivo

In a ALK+ KARPAS-299 murine xenograft model, Decitabine at a dose of 2.5 mg/kg causes increased apoptosis and reduced proliferation of tumor cells, and also results in demethylation of tumor suppressor p16INK4A. [2]

動物実験 動物モデル KARPAS-299 human cells are inoculated subcutaneously into the right and left flanks of the mice.
投与量 ≤2.5 mg/kg
投与経路 Administered via i.p.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
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 12 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

化学情報

分子量 228.21 化学式

C8H12N4O4

CAS No. 2353-33-5 SDF Download Decitabine SDFをダウンロードする
Smiles C1C(C(OC1N2C=NC(=NC2=O)N)CO)O
保管

In vitro
Batch:

DMSO : 45 mg/mL ( (197.18 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : 22.5 mg/mL

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

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よくある質問(FAQ)

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

回答
S1200 is R form

Tags: Decitabineを買う | Decitabine ic50 | Decitabine供給者 | Decitabineを購入する | Decitabine費用 | Decitabine生産者 | オーダーDecitabine | Decitabine化学構造 | Decitabine分子量 | Decitabine代理店