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Decitabine

Catalog No. T1508 CAS 2353-33-5

Synonyms: 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

Pack Size	Availability	Price/USD
50 mg	In stock	$ 30.00
100 mg	In stock	$ 39.00
200 mg	In stock	$ 59.00
500 mg	In stock	$ 122.00
1 g	In stock	$ 197.00
1 mL * 10 mM (in DMSO)	In stock	$ 43.00

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Purity: 99.87%

Purity: 99.17%

Purity: 99.14%

Purity: 99%

Biological Description

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Storage & Solubility Information

Description	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]
Kinase Assay	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].
Cell Research	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].
Animal Research	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].

Synonyms	Dacogen, NSC 127716, Deoxycytidine, 5-Aza-2'-deoxycytidine
Molecular Weight	228.21
Formula	C8H12N4O4
CAS No.	2353-33-5

Storage

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

Solubility Information

H2O: 11.4 mg/mL (50 mM)

DMSO: 55 mg/mL (241.01 mM)

References and Literature

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

Citations

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

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library EMA Approved Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library Target-Focused Phenotypic Screening Library Natural Product Library Anti-Lung Cancer Compound Library

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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

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