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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETriapineCat. No.: HY-10082CAS No.: 143621-35-6Synonyms: 3-AP; PAN-811; OCX191; NSC663249分式: CHNS分量: 195.24作靶點(diǎn): DNA/RNA Synthesis作通路: Cell Cycle/DNA Damage儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)

2、據(jù)體外實(shí)驗(yàn) DMSO : 47 mg/mL (240.73 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 5.1219 mL 25.6095 mL 51.2190 mL5 mM 1.0244 mL 5.1219 mL 10.2438 mL10 mM 0.5122 mL 2.5610 mL 5.1219 mL請(qǐng)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(chǔ)備液,并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Triapine

3、種核糖核苷酸還原酶 (ribonucleotide reductase,RR)的M2 亞基抑制劑,是有效的放射致敏劑。IC50 & Target Ribonucleotide reductase (RR) 1體外研究Triapine is a potent derivative of -heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEhRRM2 and p53R2 isoforms of the M2 subunit

4、 1. Triapine is thought to inhibit ribonucleotide reductasethrough its preformed iron chelate, rather than directly by removing iron from the active site. In cellscontaining less topoisomerase II fewer DNA strand breaks will be produced, and thus topoisomerase IIpoisons will be less inhibitory in th

5、e K/VP.5 cell line. The IC50s for Dp44mT growth inhibition are 489 nMand 6012 nM, for K562 and K/VP.5 cells, respectively. The IC50s for Triapine growth inhibition are 47639nM and 66169 nM for K562 and K/VP.5 cells, respectively 2. PKIH and DpT Fe chelators show highantiproliferative activity agains

6、t a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacywith an IC50 that ranged from 0.005 to 0.4 M. The average IC50 of Dp44mT over 28 cell types is 0.030.01M, which is significantly lower than that of Triapine (average IC50: 1.410.37 M) 3.體內(nèi)研究 Triapine causes a significant incr

7、ease (1.7-fold) in splenic weight when expressed as a percentage of totalbody weight (1.020.06%; n=25) compared with control mice (0.60.03%; n=27). In the long-term group, asignificant increase in heart weight is observed after Dp44mT (0.4 mg/kg per day) (0.80.06%; n=4)compared with control mice (0.

8、50.01%; n=6). A significant decrease in the expression of Ndrg1, TfR1, andVEGF1 in the liver is noted for Dp44mT- and Triapine (12 mg/kg per day)-treated animals. The decreasedexpression could be related to the increased liver Fe in both Dp44mT- and Triapine-treated mice 3.PROTOCOLCell Assay 2 An MT

9、T assay is used to determine cell growth inhibition of CHO cells. Human leukemia K562 cells andK/VP.5 cells (a 26-fold etoposide-resistant K562-derived sub-line with decreased levels of topoisomerase IImRNA and protein) are maintained as suspension cultures in MEM (Minimal Essential Medium Alpha,Inv

10、itrogen) containing 10% fetal calf serum (FCS). For growth inhibition assays, K562 and K/VP.5 cells areplated at a concentration of 1.5105 cell/mL, and incubated 5 d with various concentrations of Dp44mT,Triapine or vehicle (DMSO) for 48 h, after which cells are counted on a model ZBF Coulter counte

11、r. The IC50growth inhibitory concentration for each cell line is calculated from a non-linear least-squares fit to a 2-parameter logistic equation 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administration 3 Female BALB/c nu/nu mice a

12、re used at 8-10 weeks of age. Tumor cells in culture are harvested, and 107cells are suspended in Matrigel and injected s.c. into the right flanks of mice. After engraftment, tumor size ismeasured by Vernier calipers. Tumor volumes (in cubic millimeters) are calculated. When tumor volumesreached 120

13、 mm3, i.v. treatment began (day 0). Chelators (e.g., Triapine) are dissolved in 15% propyleneglycol in 0.9% saline and injected i.v. over 5 consecutive days per week for up to 7 weeks. Control mice aretreated with vehicle alone.MCE has not independently confirmed the accuracy of these methods. They

14、are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) J Mol Med (Berl). 2019 Jun 14.See more customer validations on HYPERLINK / www.MedChemE2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEREFERENCES1. Martin LK, et al. A dose escalation and pharmacodynamic study of Triapine and radiation in patients with locally adv

15、anced pancreascancer. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e475-81.2. Yalowich JC, et al. The anticancer thiosemicarbazones Dp44mT and Triapine lack inhibitory effects as catalytic inhibitors or poisons ofDNA topoisomerase II. Biochem Pharmacol. 2012 Jul 1;84(1):52-8.3. Whitnall M, et al. A class of iron chelators with a wide spectrum of potent antitumor activity that overcomes resistance tochemotherapeutics. Proc Natl Acad Sci U

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