Decitabine-NSC-127716-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDecitabineCat. No.: HY-A0004CAS No.: 2353-33-5Synonyms: NSC 127716; 5-Aza-2-deoxycytidine分式: CHNO分量: 228.21作靶点: DNA Methyltransferase作通路: Epigenetics储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protec

2、t fromlight)溶解性数据体外实验 DMSO : 50 mg/mL (219.10 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 4.3819 mL 21.9096 mL 43.8193 mL5 mM 0.8764 mL 4.3819 mL 8.7639 mL10 mM 0.4382 mL 2.1910 mL 4.3819 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药

3、式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (10.95 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (10.95 mM); Cl

4、ear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (10.95 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Decitabine (NSC 127716)种DNA甲 转移酶抑制剂，通常于治疗髓增异常综合征(MDS) 和急性髓性病 (AML)。IC50 & Target DNMT1 DNMT3A DNMT3B体外研究 Decitabine treatment signifi

5、cantly inhibits cell growth of SNU719, NCC24 and KATOIII 96 hours afterexposure to decitabine. Decitabine induces G2/M arrest and apoptosis in EBVaGC, inhibits invasion ability,and up-regulates E-cadherin expression for EBVaGC 1.Only high concentrations (10 M) Decitabine (0.1-1 M; 24-72 hours) resul

6、ts in a G2 phase arrest, which isaccompanied by a reduction of cells in G1 phase 2.Decitabine up-regulates DCTPP1 and dUTPase expression in HeLa cells 3.Cell Cycle Analysis 1Cell Line: HCT116 cellsConcentration: 0.1, 1, 10 MIncubation Time: 24, 48, 72 hoursResult: Only high drug concentrations (10 M

7、) resulted in a G2 phase arrest, which wasaccompanied by a reduction of cells in G1 phase.体内研究 Decitabine (1.0 mg/kg, p.o.) in combination with tetrahydrouridine (THU) causes severe toxicity occurs infemale CD-1 mice, and results in an increased sensitivity to decitabine toxicity correlating with de

8、citabineplasma levels 4.Decitabine (1.0 mg/kg; i.p.; once daily for 5 consecutive days) leads to regression of EL4 tumors establishedin C57BL/6 Mice 6.Animal Model: C57BL/6 mice (bearing EL4 cells) 6Dosage: 1.0 mg/kgAdministration: Intraperitoneal injection; once daily for 5 consecutive daysResult:

9、Caused continuous tumor regression even after Decitabine treatment was stopped.户使本产品发表的科研献 Ann Rheum Dis. 2019 Jun 25. pii: annrheumdis-2018-214940.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE J Allergy Clin Immunol. 2019 Jun;143(6):2038-2051.e12. Cell Death Dis. 2019 Feb 20;10(3):169. Sci Rep.

10、 2019 Jun 3;9(1):8171. Onco Targets Ther. 2018 Sep 10;11:5631-5646.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Nakamura M, et al. Decitabine inhibits tumor cell proliferation and up-regulates E-cadherin expression in Epstein-Barr virus-associatedgastric cancer. J Med Virol.

11、 2016 Jul 19.2. Hagemann S, et al. Azacytidine and decitabine induce gene-specific and non-random DNA demethylation in human cancer cell lines.PLoS One. 2011 Mar 7;6(3):e17388.3. Requena CE, et al. The nucleotidohydrolases DCTPP1 and dUTPase are involved in the cellular response to decitabine. Bioch

12、em J.2016 Jun 20.4. 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):75-85.5. Yu J, et al. DNA methyltransferase expression in triple-negative breast cancer predicts sensitivity to decitabine. J Clin Invest. 2018 Jun1;128(6):2376-2388.6. Wang LX, et al. Low dose decitabine treatment induces CD80 expression in cancer cells and stimulates tumorspecific cytotoxic Tlymphocyte responses. PLoS One. 2013 May 9;8(5):e62924.McePdfHeigh