Azacitidine (5-Azacytidine)

别名: 5-AzaC,Ladakamycin, AZA,5-Aza, CC-486,NSC 102816,5-Azacytidine 中文名称:氮胞苷, 5-氮胞苷

Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) 是胞苷的核苷类似物,通过捕获DNA甲基转移酶,特异性抑制DNA甲基化。Azacitidine可诱导线粒体凋亡与自噬。

Azacitidine (5-Azacytidine) Chemical Structure

Azacitidine (5-Azacytidine) Chemical Structure

CAS: 320-67-2

规格 价格 库存 购买数量
10mM (1mL in DMSO) 1057.59 现货
10mg 548.73 现货
50mg 788.76 现货
200mg 2212.28 现货
1g 5487.3 现货
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常与Azacitidine (5-Azacytidine)一起在实验中被使用的化合物

Venetoclax (ABT-199)


Azacitidine和Venetoclax联合治疗可显着降低从急性髓系白血病(AML)患者分离的白血病细胞中的OXPHOS水平。

Pollyea DA, et al. Nat Med. 2018 Dec;24(12):1859-1866.

Decitabine


Azacitidine和Decitabine在基因组重排过程中诱导序列元件去甲基化,导致外接合体细胞中重复元件增加。

Bracht JR, et al. Genome Biol. 2012 Oct 17;13(10):R99.

Linifanib (ABT-869)


Azacitidine和Linifanib组成的cocktail可将成纤维细胞转化为上皮样细胞,并激活OCT4。

Abbey D, et al. Cell Regen. 2022 Aug 3;11(1):27.

UNC0379


Azacitidine抑制PC9/ER和HCC827/ER细胞的细胞生长,而UNC0379对这两种细胞系的细胞生长没有显着影响。

Wang L, et al. Cell Death Dis. 2018 Jan 26;9(2):129.

Azacitidine (5-Azacytidine)相关产品

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
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
点击查看更多细胞系数据

生物活性

产品描述 Azacitidine (5-Azacytidine, 5-AzaC, Ladakamycin, AZA, 5-Aza, CC-486,NSC 102816) 是胞苷的核苷类似物,通过捕获DNA甲基转移酶,特异性抑制DNA甲基化。Azacitidine可诱导线粒体凋亡与自噬。
靶点
DNA methyltransferase [1]
(Cell-free assay)
体外研究(In Vitro)
体外研究活性

Azacitidine广泛地被用于证明特定基因区域的甲基化损失与相关基因的激活之间的相关性。Azacitidine进入到DNA后,非竞争性抑制DNA甲基化,在新复制的DNA中抑制胞嘧啶甲基化,而对休息不分裂的细胞没有抑制作用。[1] Azacitidine诱导血友病红细胞白血病细胞C3H10T1/2的分化,且诱导肌管形成。[2]Azacitidine作用于正常的真核细胞和癌细胞中,可激活核苷三磷酸,并进入DNA和RNA,抑制DNA,RNA和蛋白合成,最终导致细胞死亡。Azacitidine也抑制嘌呤代谢产物渗透到大分子中。Azacitidine抑制 L1210 细胞生长,IC50为 0.019 μg/mL [3]

细胞实验 细胞系 白血病 L1210细胞
浓度 0.15 μg/mL
孵育时间 3 天
方法

5 mL L1210 细胞(5×103cells/mL) 与药物在37°C下温育3天。使用Model A Coulter血球计数仪测定细胞数,没有测定两次,持续测定3天。

实验图片 检测方法 检测指标 实验图片 PMID
Western blot DNMT1 c-PARP / p-H2AX / H2AX 28210112
Immunofluorescence HMGB1 29097772
Growth inhibition assay Cell viability 28210112
体内研究(In Vivo)
体内研究活性

Azacitidine处理患白血病的BDF1小鼠,抑制多核苷酸合成。[3]Azacitidine 按3 mg/kg剂量腹腔注射给药 接种了Ll210腹水肿瘤细胞的患白血病的BDF1小鼠,提高平均生存时间。Azacitidine明显抑制多胺生物合成途径中所有的酶活性,包括鸟氨酸脱羧酶活性。Azacitidine 处理患白血病的小鼠,也抑制多胺的累积。[4]

动物实验 Animal Models 携带淋巴性白血病L1210的BDF1小鼠
Dosages 3 mg/kg
Administration 每天腹腔注射
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

化学信息&溶解度

分子量 244.2 分子式

C8H12N4O5

CAS号 320-67-2 SDF Download Azacitidine (5-Azacytidine) SDF
Smiles C1=NC(=NC(=O)N1C2C(C(C(O2)CO)O)O)N
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 49 mg/mL ( (200.65 mM) ;DMSO吸湿会降低化合物溶解度,请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
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

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,: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: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: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 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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