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Epigenetics
DNA Methyltransferase inhibitor
-
Apoptosis related activator
-
Nucleoside Analog/Antimetabolite inhibitor
Decitabine (5-Aza-2'-Deoxycytidine)
僅限科研使用
Decitabine (5-Aza-2'-Deoxycytidine)
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(jìn)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(xì)胞系中誘導(dǎo)細(xì)胞周期阻滯和凋亡。
Decitabine (5-Aza-2'-Deoxycytidine) Chemical Structure
CAS: 2353-33-5
產(chǎn)品質(zhì)控
批次：
純度：
99.90%
99.90
Decitabine (5-Aza-2'-Deoxycytidine)相關(guān)產(chǎn)品
| 相關(guān)靶點(diǎn) | TET DNMT1 DNMT3 | 點(diǎn)擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | RG108 SGI-1027 Zebularine (NSC 309132) Gamma-Oryzanol Bobcat339 hydrochloride β-thujaplicin CM272 GSK3685032 | 點(diǎn)擊展開 |
| 相關(guān)化合物庫(kù) | 激酶抑制劑庫(kù) FDA藥物庫(kù) 天然產(chǎn)物庫(kù) 已知活性藥物庫(kù)-I 高選擇性抑制劑庫(kù) | 點(diǎn)擊展開 |
相關(guān)信號(hào)通路圖
細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例
| 細(xì)胞系 | 實(shí)驗(yàn)類型 | 給藥濃度 | 孵育時(shí)間 | 活性描述 | 文獻(xiàn)信息(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 | ||
| 點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Decitabine是DNA甲基轉(zhuǎn)移酶抑制劑，整合進(jìn)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(xì)胞系中誘導(dǎo)細(xì)胞周期阻滯和凋亡。 | |
|---|---|---|
| 特性 | Decitabine 是DNA甲基化的有效抑制劑。 | |
| 靶點(diǎn) |
|
| 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(xì)胞時(shí)，IC50分別為 100 ng/mL 和1 ng/mL。Decitabine 抑制細(xì)胞生長(zhǎng)，這種作用存在劑量和時(shí)間依賴性，處理HL-60和KG1a白血病細(xì)胞72小時(shí)和96小時(shí)，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(xì)胞淋巴瘤(ALCL)，具有抗增殖和促凋亡活性，且抑制KARPAS-299細(xì)胞中[3H]胸甘的攝取，EC50 為0.49 μM。[2] |
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|---|---|---|---|---|
| 激酶實(shí)驗(yàn) | DNA合成檢測(cè) | |||
| 通過(guò)測(cè)定放射性胸甘攝入到DNA的情況而測(cè)定DNA合成比率。HL-60 和KG1a 細(xì)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(shí) (藥物同時(shí)加入)。48小時(shí)時(shí), 每孔加入0.5 μCi [3H] 胸甘(6.7 Ci/mmol)，再溫育24小時(shí)。細(xì)胞置于GF/C玻璃纖維過(guò)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(guò)濾器，置于EcoLite閃爍液(ICN)中，使用 Beckman LS 6000IC 閃爍計(jì)數(shù)器測(cè)量放射性。通過(guò)劑量-反應(yīng)曲線計(jì)算IC50值。 | ||||
| 細(xì)胞實(shí)驗(yàn) | 細(xì)胞系 | HL-60 和 KG1a | ||
| 濃度 | 0 到100 ng/mL | |||
| 孵育時(shí)間 | 96 小時(shí) | |||
| 方法 | 生長(zhǎng)抑制實(shí)驗(yàn)中，指數(shù)生長(zhǎng)期細(xì)胞接種在5 ml培養(yǎng)基中。向培養(yǎng)基中同時(shí)加入不同濃度Decitabine。在指定時(shí)間，使用模型 ZM Coulter 計(jì)數(shù)器對(duì)細(xì)胞進(jìn)行計(jì)數(shù)。根據(jù)藥物處理的白血病細(xì)胞的生長(zhǎng)曲線，測(cè)定IC50值。 |
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| 實(shí)驗(yàn)圖片 | 檢測(cè)方法 | 檢測(cè)指標(biāo) | 實(shí)驗(yàn)圖片 | PMID |
| Western blot | Survivin / Bcl-2 / p53 / c-Myc / DNMT1 p-AKT / AKT / p-GSK3β / GSK3β / p-Myc / Myc / p-P70 / P70 / p-4EBP-1 / 4EBP-1 / PTEN phospho-p38 / p38 / phospho-NFκB / NFκB p-JAK1 / JAK1 / p-JAK2 / JAK2 / p-STAT3 / STAT3 E-cadherin / N-cadherin / Snail / MMP-2 / MMP-9 / Bcl-2 / Bax |
|
26384351 | |
| Immunofluorescence | DNMT1 E-cadherin / MMP-9 |
|
21303982 | |
| 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(jìn)凋亡，且降低腫瘤細(xì)胞增殖，也導(dǎo)致腫瘤抑制基因p16INK4A的去甲基化。 [2] |
|
|---|---|---|
| 動(dòng)物實(shí)驗(yàn) | Animal Models | KARPAS-299 人類細(xì)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(hào) | 2353-33-5 | SDF | Download Decitabine (5-Aza-2'-Deoxycytidine) SDF |
| Smiles | C1C(C(OC1N2C=NC(=NC2=O)N)CO)O | ||
| 儲(chǔ)存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 45 mg/mL ( (197.18 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO) Water : 22.5 mg/mL (98.59 mM) Ethanol : Insoluble |
摩爾濃度計(jì)算器 |
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體內(nèi)溶解配方 現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動(dòng)物體內(nèi)配方計(jì)算器 | |||||
實(shí)驗(yàn)計(jì)算
摩爾濃度計(jì)算器
動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）
第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）
mg/kg
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μL
只
第二步：請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計(jì)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(guò)該批次藥物DMSO溶解度，請(qǐng)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(jìn)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(wèn)題及建議解決方法
問(wèn)題 1:
Is it a racemic mixture or a monomer?
回答：
Its S1200 is R form.
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