Decitabine

カタログ番号 T1508 CAS 2353-33-5

別名: Dacogen, NSC 127716, Deoxycytidine, 5-Aza-2'-deoxycytidine

Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.

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Decitabine, CAS 2353-33-5

パッケージサイズ	在庫状況	単価(税別)
サンプルについてお問い合わせ
50 mg	在庫あり	￥ 7,000
100 mg	在庫あり	￥ 9,000
200 mg	在庫あり	￥ 13,500
500 mg	在庫あり	￥ 28,000
1 g	在庫あり	￥ 45,500
1 mL * 10 mM (in DMSO)	在庫あり	￥ 10,000

バルクのお問い合わせ

バッチを選択

純度: 99.87%

COA DATASHEET SDS HPLC HNMR

純度: 99.17%

COA DATASHEET SDS HPLC HNMR

純度: 99.14%

COA DATASHEET SDS HNMR HPLC

純度: 99%

COA DATASHEET SDS HNMR

COA DATASHEET SDS

バッチの詳細情報はお問い合わせください

生物学的特性に関する説明

化学的特性

保存条件 & 溶解度情報

説明	Decitabine (Deoxycytidine) is a deoxycytidine analog, a DNA methyltransferase inhibitor with oral activity. Decitabine has antitumor activity and antimetabolic activity. Decitabine induces cell cycle arrest and apoptosis.
In vitro	METHODS: Human acute leukemia cells molt4 were treated with Decitabine (0.00625-100 μM) for 24-96 h. Cell proliferation was detected by CCK-8. RESULTS: Decitabine inhibited the proliferation of molt4 cells in a dose- and time-dependent manner, with IC50s of 84.461 μM and 10.113 μM for 72 h and 96 h treatment, respectively. [1] METHODS: Human BCP-ALL cells SEM and RS4;11 were treated with Decitabine (1000 nM) for 72 h, and the cell cycle was detected by Flow Cytometry. RESULTS: Decitabine induced G0/G1 arrest in SEM cells, and the cell cycle of RS4;11 was not affected by Decitabine. [2]
In vivo	METHODS: To assay antitumor activity in vivo, Decitabine (0.4 mg/kg) was injected intraperitoneally into NSG mice harboring the ALL tumors SEM-ffluc-GFP or RS4;11-ffluc-GFP once daily for thirty days. RESULTS: Decitabine significantly delayed leukemia cell proliferation in SEM-ffluc-GFP and RS4-ffluc-derived xenograft models. [2] METHODS: To assay anti-tumor activity in vivo, Decitabine (0.8 mg/kg) was intraperitoneally injected into Balb-c nu/nu mice harboring the human cholangiocarcinoma tumor TFK-1 once a day for fourteen days. RESULTS: In TFK-1 mouse xenografts, Decitabine delayed tumor growth and increased survival in homozygous mice. [3]
キナーゼ試験	The rate of DNA synthesis was measured by the incorporation of radioactive thymidine into DNA. HL-60 (5 × 10^3 cells/ml) and KG1a cells (10^4 cells/ml) were 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 h (drugs were added simultaneously). At 48 h, 0.5 μCi [3H] thymidine (6.7 Ci/mmol) was added to each well and incubated for an additional 24 h. The cells were 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 were then dried, placed in EcoLite scintillation liquid (ICN) and the radioactivity measured using scintillation counter. The IC50 is defined as the concentration of drug that inhibits by 50% the DNA synthesis of the leukemic cell lines from the dose-response curve [1].
細胞研究	For cell cycle analysis, KARPAS-299 cells were incubated for 24 h with 1 μM of 5-aza-CdR in RPMI and grown for 4 days in fresh RPMI only. Then, 105–106 cells were suspended in 500 μl PI-buffer (0.1% Na–citrate dihydrate, 0.1% Triton X-100, 0.1% RNAse (DNAse free) in PBS). Propidium–iodide (ROTH, dissolved in PBS) was added to a concentration of 10 μg/ml and the cells were incubated for 30 min at 37 °C. The analysis was performed on a flow cytometer using the BD FACS Diva Software. Three independent samples of 5-aza-CdR treated and PBS controls were analyzed. Descriptive statistics for analysis are reported as mean ± SEM [4].
動物実験	For xenografts, NOD.CB17-Prkdc?scid/NCrHsd (NOD/SCID, Harlan Laboratories) mice were used. KARPAS-299 human cells were grown as described above, dissolved in sterile PBS to a concentration of 1×107 cells/ml and inoculated subcutaneously (1×10^6 cells/injection) into the right and left flanks of the mice. Tumor range was followed measuring tumor length and tumor width with a calliper. Mice weighed approximately 25 g at the beginning of the therapy. 5-Aza-CdR was dissolved in sterile PBS and was administered intraperitoneally (i.p.). Each mouse received 2.5 mg/kg/mouse per treatment. Control mice were administered 100 μl of sterile PBS. Therapies were adjusted regarding start and duration of the treatment in order to obtain optimal treatment procedures. In schedule A, three mice were treated with 5-aza-CdR 11 days after inoculation, when tumor size was approximately 1 cm2. The control group contained two mice. The mice received 5-aza-CdR or PBS every day for eight days. In schedule B, two mice were treated with 5-aza-CdR three days after inoculation and three mice five days after inoculation when tumors were not or just palpable. 5-Aza-CdR was administered every other day for five times to each mouse. The control group contained two mice [4].

別名	Dacogen, NSC 127716, Deoxycytidine, 5-Aza-2'-deoxycytidine
分子量	228.21
分子式	C8H12N4O4
CAS No.	2353-33-5

保存条件

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度情報

H2O: 11.4 mg/mL (50 mM)

DMSO: 55 mg/mL (241.01 mM)

参考文献

1. Zhang G, et al. Decitabine inhibits the proliferation of human T-cell acute lymphoblastic leukemia molt4 cells and promotes apoptosis partly by regulating the PI3K/AKT/mTOR pathway. Oncol Lett. 2021 May;21(5):340. 2. Roolf C, et al. Decitabine demonstrates antileukemic activity in B cell precursor acute lymphoblastic leukemia with MLL rearrangements. J Hematol Oncol. 2018 May 4;11(1):62. 3. Wang B, et al. Decitabine inhibits the cell growth of cholangiocarcinoma in cultured cell lines and mouse xenografts. Oncol Lett. 2014 Nov;8(5):1919-1924. 4. Hassler MR, et al. Antineoplastic activity of the DNA methyltransferase inhibitor 5-aza-2'-deoxycytidine in anaplastic large cell lymphoma. Biochimie. 2012 Nov;94(11):2297-307. 5. Terse P, et al. Subchronic oral toxicity study of decitabine in combination with tetrahydrouridine in CD-1 mice. Int J Toxicol. 2014 Mar-Apr;33(2):75-85. 6. Yu J, et al. DNA methyltransferase expression in triple-negative breast cancer predicts sensitivity to decitabine. J Clin Invest. 2018 Jun 1;128(6):2376-2388. 7. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination[J]. Antiviral Research. 2020: 104931 8. Chen G, Fan X, Li Y, et al. Promoter aberrant methylation status of ADRA1A is associated with hepatocellular carcinoma[J]. Epigenetics. 2020: 1-18. 9. Fan X, Li Y, Yi X, et al. Epigenome-wide DNA methylation profiling of portal vein tumor thrombosis (PVTT) tissues in hepatocellular carcinoma patients[J]. Neoplasia. 2020, 22(11): 630-643. 10. Zhang M, Wang L, Yue Y, et al. ITPR3 Facilitates Tumor Growth, Metastasis and Stemness by Inducing the NF-ĸB/CD44 Pathway in Urinary Bladder Carcinoma[J]. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-20

引用文献

1. Chen Y, Li K, Gong D I, et al. ACLY: A biomarker of recurrence in breast cancer. Pathology-Research and Practice. 2020, 216(9): 153076 2. Zhang M, Wang L, Yue Y, et al. ITPR3 Facilitates Tumor Growth, Metastasis and Stemness by Inducing the NF-ĸB/CD44 Pathway in Urinary Bladder Carcinoma. Journal of Experimental & Clinical Cancer Research. 2021, 40(1): 1-20 3. Fan X, Li Y, Yi X, et al Epigenome-wide DNA methylation profiling of portal vein tumor thrombosis (PVTT) tissues in hepatocellular carcinoma patients. Neoplasia. 2020, 22(11): 630-643 4. Thieulent C, Hue E, Sutton G, et al. Identification of antiviral compounds against equid herpesvirus-1 using real-time cell assay screening: efficacy of decitabine and valganciclovir alone or in combination. Antiviral Research. 2020: 104931 5. Zhou H, Ning Y, Zeng G, et al. Curcumin promotes cell cycle arrest and apoptosis of acute myeloid leukemia cells by inactivating AKT. Oncology Reports. 2021, 45(4): 1-1. 6. Fan X, Guo H, Dai B, et al. The association between methylation patterns of DNAH17 and clinicopathological factors in hepatocellular carcinoma. Cancer Medicine. 2019 Jan;8(1):337-350 7. Łagosz-Ćwik K, Melnykova M, Nieboga E, et al.Mapping of DNA methylationsensitive cellular processes in gingival and periodontal ligament fibroblasts in the context of periodontal tissue homeostasis.Frontiers in Immunology.2023, 14. 8. He S, Li Y, Shi X, et al.DNA methylation landscape reveals LIN7A as a decitabine-responsive marker in patients with t (8; 21) acute myeloid leukemia.Clinical Epigenetics.2023, 15(1): 1-13. 9. He S, Li Y, Wang L, et al.DNA methylation landscape reveals GNAS as a decitabine-responsive marker in patients with acute myeloid leukemia.Neoplasia.2024, 49: 100965. 10. Hoang N M, Liu Y, Bates P D, et al.Targeting DNMT3A-mediated oxidative phosphorylation to overcome ibrutinib resistance in mantle cell lymphoma.Cell Reports Medicine.2024

投与量変換

You can also refer to dose conversion for different animals. 詳細

In vivo投与量計算 (透明溶液)

ステップ1: 以下の情報を入力してください

投与量

mg/kg

動物の平均体重

動物あたりの投与量

動物数

溶媒の組成を入力してください

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

計算するリセット

計算結果:

作業濃度: mg/ml;

DMSO溶液の作成方法: mg あらかじめ溶解した薬剤 μL DMSO (マスター溶液の濃度 mg/mL)，濃度がそのバッチの薬剤のDMSO溶解度を超える場合は、まずご連絡ください。

生体内薬剤の調合法：取る μL DMSO マスター溶液、次に追加 μL PEG300，確実に混ぜてから加える μL Tween 80，確実に混ぜてから加える μL ddH₂O, 確実に混ぜる

お問合せ内容:

必ず順番通りに溶媒を加えてください。ボルテックスミキサーや超音波、湯煎することで溶解しやすくなります

計算器

モル濃度計算機

希釈計算機

再構成計算

分子量計算機

質量

濃度

体積

分子量

モル度計算機では以下の計算が可能です

既知の体積と濃度の溶液を調製するために必要な化合物の質量
質量が既知の化合物を目的の濃度まで溶解させるのに必要な溶液の量
特定の体積の中に既知の質量の化合物を入れて得られる溶液の濃度

参考例

モル濃度計算機を使用したモル濃度計算の例
化合物の分子量が197.13g/molである場合、10mlの水に10mMのストック溶液を作るのに必要な化合物の質量はどれくらいですか？
［分子量（MW）］の欄に［197.13］と入力してください
[濃度]ボックスに10と入力し、正しい単位（millimolar）を選択します
[容量]ボックスに10と入力し、正しい単位（milliliter）を選択します
計算を押します
答えの19.713mgが質量欄に表示されます

濃度 (開始)

体積 (開始)

濃度 (終了)

体積 (終了)

溶液を作るのに必要な希釈率の計算

溶液の調製に必要な希釈率の算出
希釈計算機は、既知の濃度の原液をどのように希釈するかを計算することができる便利なツールです。V1を計算するためにC1、C2＆V2を入力します。

参考例

Tocrisの希釈計算器を用いた希釈計算の一例
50μMの溶液を20ml作るためには、10mMの原液を何ml必要ですか？
C1V1=C2V2という式を用いて、C1=10mM、C2=50μM、V2=20ml、V1を未知数とします。
濃度（開始）ボックスに10を入力し正しい単位(millimolar)を選択してください
濃度（終了）ボックスに50を入力し正しい単位(millimolar)を選択してください
体積（終了）ボックスに20を入力し正しい単位(millimolar)を選択してください
計算を押します
100 microliter (0.1 ml) という答えが体積（開始）ボックスに表示されます。

分子式

分子量 g/mol

化合物の化学式を入力して、そのモル質量や元素組成を計算します

Tヒント：化学式は大文字と小文字を区別します。: C10H16N2O2 c10h16n2o2

化合物のモル質量（分子量）を計算する手順:
化学物質のモル質量を計算するには、その化学式を入力し、「計算」をクリックしてください。.
分子質量、分子量、モル質量、モル重量の定義:
分子質量（分子量）とは、物質の1分子の質量であり、統一された原子質量単位（u）で表されます。(1uは炭素12の1原子の質量の1/12に等しい）
モル質量（molar weight）とは、ある物質の1モルの質量のことで、単位はg/molです。

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技術サポート

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Decitabine 2353-33-5 Apoptosis Cell Cycle/Checkpoint Chromatin/Epigenetic DNA Damage/DNA Repair Nucleoside Antimetabolite/Analog DNA Methyltransferase DNMTs NSC-127716 Dacogen inhibit NSC 127716 DNA MTases NSC127716 Deoxycytidine 5-Aza-2'-deoxycytidine Inhibitor inhibitor

本ウェブサイトに掲載されている製品は全て研究用試薬です。研究目的以外の用途にはご使用できません。

Decitabine

保存条件

溶解度情報

参考文献

引用文献

関連化合物ライブラリー

関連製品

投与量変換

In vivo投与量計算 (透明溶液)

計算器

モル度計算機では以下の計算が可能です

溶液を作るのに必要な希釈率の計算

バイアルを再構成するのに必要な溶媒の量を計算する.

化合物の化学式を入力して、そのモル質量や元素組成を計算します

技術サポート

Keywords