替尼泊苷作用機(jī)制 - Medchemexpress - MCE中國

1、Product Data SheetTeniposideCat. No.: HY-13761CAS No.: 29767-20-2分式: CHOS分量: 656.65作靶點(diǎn): Topoisomerase作通路: Cell Cycle/DNA Damage儲存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect from light)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 30 mg/mL (45.69 mM)* means soluble, but saturation unknown.Solve

2、ntMass1 mg 5 mg 10 mgConcentration制備儲備液1 mM 1.5229 mL 7.6144 mL 15.2288 mL5 mM 0.3046 mL 1.5229 mL 3.0458 mL10 mM 0.1523 mL 0.7614 mL 1.5229 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲備液的保存式和期限：-80C, 6 months; -20C, 1 month (protect from light)。-80C 儲存時(shí)，請?jiān)?6 個(gè)內(nèi)使，-20C 儲存時(shí)，請?jiān)?1 個(gè)內(nèi)使。體內(nèi)實(shí)驗(yàn)

3、請根據(jù)您的實(shí)驗(yàn)動物和給藥式選擇適當(dāng)?shù)娜芙獍?。以下溶解案都請先按?In Vitro 式配制澄清的儲備液，再依次添加助溶劑：為保證實(shí)驗(yàn)結(jié)果的可靠性，澄 的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天 使； 以下溶劑前顯的百分 指該溶劑在您配制終溶液中的體積占；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可 以通過加熱和/或超聲的式助溶1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.81 mM); Clear solution此案可獲得 2.5 mg/mL (3.81 m

4、M，飽和度未知) 的澄清溶液。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄 DMSO 儲備液加到 400 L PEG300 中，混合均勻；向上述體系中加50 L Tween-80，混合均勻；然后繼續(xù)加 450 L 理鹽定容 1 mL。2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.81 mM); Clear solution此案可獲得 2.5 mg/mL (3.81 mM，飽和度未知) 的澄 溶液，此案不適于實(shí)驗(yàn)周 期在半個(gè)以上的實(shí)驗(yàn)。以 1 mL 作液為例，取 100 L 25.0 mg/mL 的澄

5、 DMSO 儲備液加到 900 L 油中，混合均勻。Page 1 of 2 www.MedChemEBIOLOGICAL ACTIVITY物活性 Teniposide種葉草毒素衍物， 拓?fù)洚悩?gòu)酶 II (topoisomerase II) 的抑制劑，同時(shí)為種化療劑。IC & Target Topoisomerase II體外研究 Teniposide is a topoisomerase II inhibitor. Teniposide (VM-26, 0.15-45 mg/L) inhibits the proliferation of Tca8113 cellsin a dose-depe

6、ndent manner, with an IC50 of 0.35 mg/L. Teniposide (5 mg/L) induces apoptosis of Tca8113 cells.Teniposide (5.0 mg/L) causes cell arrested at G2/M phase in Tca8113 cells2. Teniposide is active on primary culturedglioma cells from patients, when the level of miR-181b is high in the cells, with an IC5

7、0 of 1.3 0.34 g/mL. Cellstreated with teniposide with low MDM2 have decreased viability compared with control cells, and the IC50 decreasesfrom 5.86 0.36 g/mL to 2.90 0.35 g/mL upon MDM2 suppression. Teniposide also inhibits the viability of gliomacell with high level of miR-181b, through mediation

8、of MDM23.體內(nèi)研究 Teniposide (0.5 mg/kg, i.p.) significantly increases micronucleated polychromatic erythrocyte (MNPCE) frequencies, which is directly related to bone marrow toxicity as significant suppression of bone marrow is noted. Teniposide (24 mg/kg, i.p.) markedly decreases the frequencies of Brd

9、U-labelled sperm. Teniposide (12, 24 mg/kg, i.p.) alsodramatically induces disomic sperm in the germ cell of male mice1.PROTOCOLCell Assay 2 Logarithmically growing Tca8113 cells are trypsinized and made into single cell suspension then plated in 96-wellculture plate at a concentration of 5 104 cell

10、s/well, eight columns for Teniposide and seven columns for CDDP ineach plate, 3 wells in each column. After 24 hours of incubation, the medium of the 3 wells in each column arereplaced with medium containing Teniposide of 0.15 mg/L, 0.5 mg/L, 1.5 mg/L, 5.0 mg/L, 15 mg/L and 45 mg/L orCDDP of 0.1 mg/

11、L, 0.3 mg/L, 1.0 mg/L, 3.0 mg/L and 9.0 mg/L, respectively. Blank control wells are added mediumwithout drugs. Cells are then cultured for another 24 hours, 48 hours, 72 hours, 96 hours and 120 hours. Thesupernatants are removed and 20 L MTT solution is added in each well, followed with another 4 ho

12、urs of culture.The supernatants are discarded carefully and 200 L dimethyl sulphoxide (DMSO) is added and shaken vigorously todissolve the purple precipitation formation. Optical density (OD) of each well is tested using Spectrophotometer witha wavelength of 450 nm. The experiment is repeated in tri

13、plicate2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Animals (mice) are treated with 0.5 mg/kg teniposide and bone marrow is sampled 24 h after treatment. ColchicineAdministration 1 and mitomycin C are used as a positive control aneugen and c

14、lastogen, respectively, at the dose of 2 mg/kg each.Bone marrow smears are prepared and stained with May-Gruenwald/Giemsa solutions. At least four slides are madefor each animal and allowed to dry overnight. One slide per animal is stained with May-Gruenwald/Giemsa solutionsfor conventional assessme

15、nt of the micronuclei (MN) frequencies in polychromatic erythrocytes (PCEs) andnormochromatic erythrocytes (NCEs). The remaining unstained slides are stored at 20C for the distinction betweenthe clastogenic and aneugenic effects by identifying the origin of MN with the mouse DNA probes. Per animal,

16、1000PCE of coded slides are scored for the presence of MN. In addition, the number of PCEs among 1000 NCE per animalis recorded to evaluate bone marrow suppression and mitotic activity is calculated as %PCE = PCE/(PCE + NCE) 1001.MCE has not independently confirmed the accuracy of these methods. The

17、y are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn)Page 2 of 3 www.MedChemE J Mol Med (Berl). 2019 Aug;97(8):1183-1193. Acta Pharmacol Sin. 2020 May 12.See more customer validations on HYPERLINK www.MedChemE www.MedChemEREFERENCES1. Attia SM, et al. Molecular cytogenetic evaluation of the aneugenic effects of teni

18、poside in somatic and germinal cells of male mice. Mutagenesis. 2012Jan;27(1):31-9.2. Li J, et al. Topoisomerase II trapping agent teniposide induces apoptosis and G2/M or S phase arrest of oral squamous cell carcinoma. World J SurgOncol. 2006 Jul 6;4:41.3. Sun YC, et al. MiR-181b sensitizes glioma cells to teniposid