Datelliptium-chloride-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDatelliptium chlorideCat. No.: HY-U00337CAS No.: 105118-14-7分式: CHClNO分量: 397.94作靶点: DNA/RNA Synthesis作通路: Cell Cycle/DNA Damage储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 H2O : 41.67 mg/mL (1

2、04.71 mM; Need ultrasonic)DMSO : 1 mg/mL (insoluble or slightly soluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5129 mL 12.5647 mL 25.1294 mL5 mM 0.5026 mL 2.5129 mL 5.0259 mL10 mM 0.2513 mL 1.2565 mL 2.5129 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。BIOLOGICAL ACTIVITY物活性 Datellipti

3、um chloride种源于 ellipticine 的 DNA 嵌合剂，具有抗肿瘤活性。体外研究Datelliptium (100 M) shows significantly cytotoxic effects after 2 hr of treatment in suspension and primarycultures of rat hepatocytes. Datelliptium mobilizes glycogen in both rat systems in vitro concentrationdependently. The half-maximal effect is

4、14.3 M in isolated hepatocytes, whereas in cultured rat hepatocytesit is 5.9 M. Datelliptium also leads to a concentration-dependent decrease in gluconeogenesis from lactate1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEin cells 1. Datelliptium acetate is selectively cytotoxic for solid tumors ove

5、r leukemia L1210. Human tumorsH-125 and HCT-116 demonstrates less sensitivity to datelliptium acetate 2.体内研究 Upon intravenous administration, datelliptium acetate shows potent inhibitory activities in vivo against avariety of murine solid tumors. Datelliptium acetate is highly active against early-s

6、tage colon #38 with highestnon-toxic dose (HNTD) of 170 mg/kg TD, and weight loss of 10%, T/C of 0% 2.PROTOCOLCell Assay 1 Cytotoxicity is estimated after short-term exposure (2 hr) to datelliptium using suspended and cultured rathepatocytes. When cytotoxicity is evaluated after longer-term exposure

7、, using human and rat monolayersand hepatoma cell lines, the compound is added 1 hr after cell plating and incubated for 23 hr. The loss ofintracellular LDH and the MTT test are the endpoints evaluated in cultured cells. The intracellular LDH ismeasured in the microwell culture plates by a colorimet

8、ric method. The MTT test, reduction of the tetrazoliumsalt MTT to formazan by mitochondrial succinate dehydrogenase, is performed as described. Cytotoxicity inthe hepatocyte suspension is evaluated by LDH leakage to the medium after a 2-hr treatment with the drug.MCE has not independently confirmed

9、the accuracy of these methods. They are for reference only.REFERENCES1. Donato MT, et al. Toxicity of the antitumoral drug datelliptium in hepatic cells: Use of models in vitro for the prediction of toxicity in vivo.Toxicol In Vitro. 1992 Jul;6(4):295-302.2. Mucci-LoRusso P, et al. Activity of datelliptium acetate (NSC 311152; SR 95156A) against solid tumors of mice. Invest New Drugs. 1990Aug;8(3):253-61.McePdfHeightCaution: Product has not been fully validated for