ホームページ DNA Damage/DNA Repair DNA Methyltransferase inhibitor - Nucleoside Analog/Antimetabolite chemical - Autophagy activator Azacitidine (5-Azacytidine) For research use only.

Azacitidine (5-Azacytidine)

別名：5-AzaC,Ladakamycin, AZA,5-Aza, CC-486,NSC 102816,5-Azacytidine

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.

Azacitidine (5-Azacytidine)化学構造

CAS No. 320-67-2

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 44500 国内在庫あり
JPY 71500 国内在庫あり
JPY 145500 国内在庫あり

代表番号: 045-509-1970|電子メール：[email protected]
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製品安全説明書

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Azacitidine (5-Azacytidine)関連製品

シグナル伝達経路

DNA Methyltransferase Signaling Pathways

DNA Methyltransferaseシグナル伝達経路

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
OCM1 Function Assay 0.5/1 μM 48 h causes global DNA hypomethylation at L-1 repeat loci 25146981
92.1 Cell Viability Assay 0.5/1 μM 5 d decreases radiation-induced cell viability inhibition 25146981
OCM1 Cell Viability Assay 0.5/1 μM 5 d decreases radiation-induced cell viability inhibition 25146981
OMM1 Function Assay 0.5/1 μM 48 h decreases invasion dose dependently  25146981
Mel 290 Function Assay 0.5/1 μM 48 h decreases invasion dose dependently  25146981
OCM3 Function Assay 0.5/1 μM 48 h decreases invasion dose dependently  25146981
Mel 290 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
Mel 285 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
OMM1 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
OCM1 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
92.1 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
OCM3 Function Assay 0.5/1 μM 48 h decreases clonogenicity dose-dependently 25146981
Mel 290 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
Mel 285 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
OMM1 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
OCM1 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
92.1 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
OCM3 Growth Inhibition Assay 0.5/1/2 μM 7 d inhibits cell growth in a dose dependent manner 25146981
CP70 Function Assay 5 µM  7 d weakens the level of methylation 25299694
A2780 Function Assay 5 µM  7 d weakens the level of methylation 25299694
CP70 Function Assay 5 µM  7 d increases DNA methylation level 25299694
A2780 Function Assay 5 µM  7 d increases DNA methylation level 25299694
MV4-11 Function Assay 5 μM 72 h significantly upregulates ZNF382 expression 25319049
HL-60 Function Assay 5 μM 72 h significantly upregulates ZNF382 expression 25319049
MSCs Function Assay 10 μM 24 h promotes the commitment of MSCs to myocardial differentiation 25351395
HRPE Function Assay 5/10 μM 48 h down-regulates of VEGF, IL-1β, and MMP2 dose-dependently 25352747
HREC Function Assay 5/10 μM 48 h down-regulates of VEGF, ICAM-1 (not protein level in HRPE cells), IL-1β dose-dependently 25352747
HRPE Function Assay 5/10 μM 48 h induces PEDF in a dose-dependent manner 25352747
HREC Function Assay 5/10 μM 48 h induces PEDF in a dose-dependent manner 25352747
MKN45 Function Assay 5 μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
SGC-7901 Function Assay 5 μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
MKN28 Function Assay 5 μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
BGC-823 Function Assay 5 μM 72 h decreases the mRNA expression of PRL-3 significantly 25475733
MKN45 Function Assay 5 μM 72 h decreases the PRL-3 protein level signifcantly 25475733
SGC-7901 Function Assay 5 μM 72 h decreases the PRL-3 protein level signifcantly 25475733
MKN28 Function Assay 5 μM 72 h decreases the PRL-3 protein level signifcantly 25475733
BGC-823 Function Assay 5 μM 72 h decreases the PRL-3 protein level signifcantly 25475733
MCF7 Growth Inhibition Assay 0.3 μM  4 d decreases the cell growth 24.8% combined with GSK126 25477340
PC3 Growth Inhibition Assay 0.2 μM  4 d decreases the cell growth to 20.3% combined with GSK126 25477340
MCF7 Function Assay 0.3 μM  4 d increases the gene expression of IGFBP7, SFRP1 and SLC6A15 combined with GSK126 25477340
PC3 Function Assay 0.2 μM  4 d increases the gene expression of IGFBP7, SFRP1 and SLC6A15 combined with GSK126 25477340
A253 Function Assay 10 µM 0-4 d reduces the 5-methylcytosine content 25485536
A253 Function Assay 10 µM 72 h increases the expression level of the M3R in both membrane and cytosolic preparations 25485536
A253 Function Assay 10 µM 0-4 d increases the mRNA expression level of the M3R after 24 h 25485536
Ketr-3 Function Assay 10 µM 72 h induces the ADAMTS18 gene expression 25569086
CaKI-2 Function Assay 10 µM 72 h induces the ADAMTS18 gene expression 25569086
A498 Function Assay 10 µM 72 h induces the ADAMTS18 gene expression 25569086
MDA-MB-231  Function Assay 1/2.5/5 μM 24/48 h increases the expression of miRNA-124 at the concerntration of 5 μM 25817229
MCF-7 Function Assay 1/2.5/5 μM 24/48 h increases PARP cleavage  25817229
MDA-MB-231 Function Assay 1/2.5/5 μM 24/48 h induces significant PARP cleavage after 48 h 25817229
MDA-MB-231 Function Assay 1/2.5/5 μM 48 h increases the levels of E-cadherin mRNA at the concerntration of 2.5 μMfor 48 h 25817229
MDA-MB-231 Function Assay 1/2.5/5 μM 48 h decreases the PTPN12 expression at the concerntration of 5 μM 48 h 25817229
Jurkat  Function Assay 3.5 µM 48 h increases PTPL1 mRNA expression 26133246
Raji  Function Assay 15 µM 48 h increases PTPL1 mRNA expression 26133246
CA46 Function Assay 20 µM 48 h increases PTPL1 mRNA expression 26133246
Jurkat  Growth Inhibition Assay 0.1-50 μM 12-72 h inhibits cell growth in a dose dependent manner 26133246
Raji  Growth Inhibition Assay 0.1-50 μM 12-72 h inhibits cell growth in a dose dependent manner 26133246
OCM3 Function Assay 0.5/1 μM 48 h causes global DNA hypomethylation at L-1 repeat loci 25146981
92.1 Function Assay 0.5/1 μM 48 h causes global DNA hypomethylation at L-1 repeat loci 25146981
IMR32 Function Assay 3 μM 72 h induces p19-INK4d expression significantly 25104850
IMR5-75 Function Assay 3 μM 72 h induces p19-INK4d expression significantly 25104850
Be(2)-C Function Assay 3 μM 72 h induces p19-INK4d expression significantly 25104850
Bxpc-3 Growth Inhibition Assay 5/10 μM 24/48/72 h inhibits the proliferation of Bxpc-3 cells in time- and concentration-dependent manners 25061731
Bxpc-3 Apoptosis Assay 5/10 μM 24/48/72 h induces apoptosis in time- and concerntration manners 25061731
Bxpc-3 Function Assay 5/10 μM 24/48/72 h decreases β-catenin expression after 24 h 25061731
Bxpc-3 Function Assay 5/10 μM 24/48/72 h decreases cyclinD1 expression at the concerntration of 10 μM 25061731
Bxpc-3 Function Assay 5/10 μM 24/48/72 h down-regulateS c-myc mRNA expression in time- and concentration-dependent manners 25061731
HL-60 Growth Inhibition Assay 1.0 μM 48 h significantly inhibits HL-60 cell growth  25051119
HL-60 Function Assay 1.0 μM 48 h increases p21WAF1/CIP1 and caspase-3 expression  25051119
HL-60 Function Assay 1.0 μM 48 h decreases Bcl-xL expression significantly 25051119
HuTu-80  Function Assay 1/5/10 μM 48/72 h increases the expression of human NPC1L1 mRNA in a dose-dependent manner 24904062
Caco2  Function Assay 10 μM 48 h increases NPC1L1 expression 24904062
HepG2  Function Assay 0-25 μM 24 h decreases subtilisin/kexin type 9 (PCSK9) protein levels dose dependently 24855646
HepG2  Function Assay 0-25 μM 24 h increases low density lipoprotein receptor (LDLR) gene expression  24855646
HepG2  Function Assay 10 μm  0-24 h decreases PCSK9 and HMGCR expression and increases LDLR expression after 6 h 24855646
HepG2  Function Assay 10 μm 24 h promotes cytosolic neutral lipid accumulation independently of exogenous lipoproteins 24855646
HepG2  Function Assay 10 μm 24 h prevents SREBP processing 24855646
HC45  Function Assay 5µM  4 d reduces the methylation levels of WIF1, P16, CXCL14, NKX2–3, CDH1, LAMA1, and CTNNB1 24762809
CNDT2  Function Assay 5µM  4 d reduces the methylation levels of WIF1, P16, CXCL14, NKX2–3, CDH1, LAMA1, and CTNNB1 24762809
CNDT2  Function Assay 5µM  4 d increases gene expression of WIF1, P16, CDH1, LAMA1, and CTNNB1 24762809
T-cells Growth Inhibition Assay 5/20 μM 0-48 h inhibits cell growth in a dose dependent manner 24757283
CD3+ T-cells Function Assay 5/20 μM 48 h upregulates p15 expression 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h upregulates p15 expression 24757283
CD8+ T-cells Function Assay 5/20 μM 48 h upregulates p15 expression 24757283
CD3+ T-cells Function Assay 5/20 μM 48 h upregulates the expression of FOXP3 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h upregulates the expression of FOXP3 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h reduces TBET1 mRNA expression 24757283
CD4+ T-cells Function Assay 5/20 μM 48 h upregulates the expression of RORγt  24757283
CD4+ T-cells Function Assay 5/20 μM 48 h inhibits memory T-cells 24757283
CD8+ T-cells Function Assay 5/20 μM 48 h inhibits memory T-cells 24757283
CD3+ T-cells Function Assay 5 μM 48 h reduces long-term memory cell phenotype 24757283
U937 Apoptosis Assay 10 μM 72 h induces apoptosis significantly 24680865
HL-60 Apoptosis Assay 10 μM 72 h induces apoptosis significantly 24680865
MCF7 Function Assay 5 μM 48 h  displays selective toxicity toward suspended MCF-7 cells 24633350
MCF7 Function Assay 10 μM 24 h  induces the cleavage of caspase 7 and PARP  24633350
MCF7 Function Assay 0–0.5 μM  7 d inhibits the growth MCF-7 tumorspheres in suspension cultures  24633350
MCF7 Function Assay 0.5 μM  14 d reduces the size of MCF-7 colonies embedded in soft agar 24633350
MCF7 Function Assay 0.05–20 μM 1 d reduces the clonal survival of MCF-7 cells in monolayer cultures 24633350
T47D  Function Assay 0.5 μM 4 d inhibits tumorsphere formation 24633350
MCF7 Function Assay 0.5–10 μM 48 h  inhibits the gap closure in the wound healing assay 24633350
MCF7 Function Assay 0/10 μM 24 h inhibits the activity of MMP9 24633350
MDA-MB-231  Function Assay 0.5–10 μM 36 h inhibits the migration 24633350
U373-MAGI Antiviral assay 25 to 400 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 25 to 400 uM after 2 to 72 hrs by qPCR method 27117260
U373-MAGI Antiviral assay 25 to 400 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 25 to 400 uM after 2 to 72 hrs by qPCR method 27117260
MCF7 Function assay 15 uM 72 hrs Inhibition of UHRF1 in human MCF7 cells assessed as decrease in methylation at RAR beta exon at 15 uM after 72 hrs by methylation specific-PCR method 27049577
SKM1-S Apoptosis assay 1 uM Induction of apoptosis in human SKM1-S cells assessed as caspase 3 cleavage at 1 uM by Western blot method 28094938
SKM1-S Antiproliferative assay 48 hrs Antiproliferative activity against human SKM1-S cells after 48 hrs by XTT assay, IC50 = 0.5 μM. 28094938
SKM1-S Antiproliferative assay 48 hrs Antiproliferative activity against human SKM1-S cells after 48 hrs by DAPI-staining-based flow cytometric method, EC50 = 0.51 μM. 28094938
A427 Antiproliferative assay 96 hrs Antiproliferative activity against human A427 cells after 96 hrs by crystal violet assay, IC50 = 0.63 μM. 18434163
KYSE70 Antiproliferative assay 96 hrs Antiproliferative activity against human KYSE70 cells after 96 hrs by crystal violet assay, IC50 = 1.59 μM. 18434163
5637 Antiproliferative assay 96 hrs Antiproliferative activity against human 5637 cells after 96 hrs by crystal violet assay, IC50 = 1.73 μM. 18434163
HT-29 Antiproliferative assay 96 hrs Antiproliferative activity against human HT-29 cells after 96 hrs by MTT assay, IC50 = 3.8 μM. 2778449
P388 Antiproliferative assay 48 hrs Antiproliferative activity against mouse P388 cells after 48 hrs by MTT assay, IC50 = 5 μM. 2778449
MCF7 Antiproliferative assay 96 hrs Antiproliferative activity against human MCF7 cells after 96 hrs by crystal violet assay, IC50 = 6.78 μM. 18434163
L1210 Cytotoxicity assay Cytotoxicity against mouse L1210 cells assessed as cessation of growth 69026
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells 29435139
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明 Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) is a nucleoside analogue of cytidine that specifically inhibits DNA methylation by trapping DNA methyltransferases. Azacitidine induces mitochondrial apoptosis and autophagy.
Targets
DNA methyltransferase [1]
(Cell-free assay)
In Vitro
In vitro

Azacitidine is widely used to demonstrate the correlation between loss of methylation in specifc gene regions and activation of the associated genes. After incorporation into DNA, Azacitidine inhibits DNA methyltransferase noncompetitively, causing a block in cytosine methylation in newly replicated DNA but not in resting, nondividing cells. [1] Azacitidine induces differentiation of Friend Erythroleukemia Cell C3H10T1/2 with myotube formation. [2] Azacitidine can be activated to the nucleoside triphosphate and incorporate into both DNA and RNA, leading to inhibition of DNA, RNA and protein synthesis in normal eukaryotic cells and in cancer cell lines, which could finally leads to cell death. Azacitidine also inhibits the incorporation of purine metabolites into macromolecules. Azacitidine inhibits the L1210 cells growth with IC50 and of 0.019 μg/mL. [3]
細胞実験 細胞株 Leukemia L1210 cell
濃度 0.15 μg/mL
反応時間 3 days
実験の流れ

5 mL of L1210 cells (5 × 103 cells/mL) are incubated with Azacitidine at 37 ℃ for 3 days. Cell number is determined twice a day for 3 days by means of a Model A Coulter counter.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot DNMT1 c-PARP / p-H2AX / H2AX 28210112
Immunofluorescence HMGB1 29097772
Growth inhibition assay Cell viability 28210112
In Vivo
In Vivo

Azacitidine inhibits polynucleotide synthesis in leukemic BDF1 mice. [3] Azacitidine (3 mg/kg, i.p.) increases the mean survival time in leukemic BDF1 mice inoculated with Ll210 ascites tumor cells. Azacitidine markedly suppresses all enzymes activity in the polyamine-biosynthetic pathway, including ornithine decarboxylase activity. putrescine-dependent S-adenosyl-L-methionine decarboxylase activity, and spermidine-dependent S-adenosyl-L-methionine decarboxylase activity. Azacitidine also inhibits the accumulations of polyamines in leukemic mice. [4]
動物実験 動物モデル BDF1 mice bearing lymphoid leukemia L1210
投与量 3 mg/kg
投与経路 Daily i.p. injection
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06372717 Not yet recruiting
Acute Myeloid Leukemia Refractory|Myelodysplastic Syndrome Acute Myeloid Leukemia|Myelodysplastic Syndrome With Excess Blasts|Acute Myeloid Leukemia in Relapse
Apollo Therapeutics Ltd
 April 2024 Phase 1|Phase 2
NCT06263387 Not yet recruiting
AML Adult
French Innovative Leukemia Organisation|Acute Leukemia French Association
 April 29 2024 --
NCT06159491 Not yet recruiting
Chronic Myelomonocytic Leukemia
Douglas Tremblay|Sobi Inc.|Icahn School of Medicine at Mount Sinai
 January 2 2024 Phase 1|Phase 2
NCT06022003 Recruiting
AML Adult|Refractory AML|Relapsed Adult AML|FLT3-TKD Mutation|FLT3-ITD
French Innovative Leukemia Organisation|Acute Leukemia French Association
 January 13 2024 Phase 2
NCT06014489 Recruiting
AML Adult
Stichting Hemato-Oncologie voor Volwassenen Nederland
 January 17 2024 Phase 2

化学情報

分子量 244.2 化学式

C8H12N4O5
CAS No. 320-67-2 SDF Download Azacitidine (5-Azacytidine) SDFをダウンロードする
Smiles C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N
保管

In vitro
Batch:

DMSO : 49 mg/mL ( (200.65 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 : Insoluble

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 匹

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。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

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よくある質問（FAQ）

質問1:
Is the vehicle (30% Propylene glycol, 5% Tween 80, 65% D5W) for Azacitidine (Catalog No.S1782) safe for subcutaneous dosing?

回答
S1782 in 30% Propylene glycol+5% Tween 80+65% D5W at 30mg/ml is a suspension. If you are going to administrate this compound for oral gavage, it is fine. But if you administrate the drug via injection, you need a clear solution and S1782 can be dissolved in 5% DMSO+30% PEG 300+ddH2O at 10mg/ml clearly.

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