Daun02 - Topoisomerase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDaun02Cat. No.: HY-13061CAS No.: 290304-24-4分式: CHNO分量: 884.79作靶點(diǎn): Topoisomerase; ADC Cytotoxin作通路: Cell Cycle/DNA Damage; Antibody-drug Conjugate/ADCRelated儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶

2、解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 100 mg/mL (113.02 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.1302 mL 5.6511 mL 11.3021 mL5 mM 0.2260 mL 1.1302 mL 2.2604 mL10 mM 0.1130 mL 0.5651 mL 1.1302 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。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配?/p>

3、前請(qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (2.83 mM); Clear solutionBIOLOGICAL ACTIVITY1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Daun02是拓?fù)洚悩?gòu)酶抑制劑Daunorubici

4、n的前藥。IC50 & Target Topoisomerase體外研究 Daun02 is a prodrug, which is converted by -galactosidase to Daunorubicin, which has been shown to reducecalcium ion (Ca2+)-dependent action potentials in neuroblastoma cells 1. Daunorubicin is a topoisomeraseinhibitor 2. Daun02 is a good substrate for -galactosi

5、dase (-gal). The concentration of Daun02 producing50% (EC50) decrease in cell viability is 0.5 M, 1.5 M, and 3.5 M for T47-D, Panc02, and MCF-7,respectively 3.體內(nèi)研究 Daun02 is a good substrate for -gal with Km and Vmax values of 0.37 mM and 8.6 mol/min/mg protein. At aconcentration of 10-5 M, Daun02 i

6、s 79% bound to plasma protein compares to 94% for Daunomycin 3.PROTOCOLCell Assay 3 Murine Panc02 cells are maintained as exponentiallygrowing monolayer cultures in DMEM/F12 or RPMI-1640 medium supplemented with 10% FBS, 1% glutamine, penicillin, and streptomycin at 37C. Forcytotoxicity assay, the c

7、ells are seeded into 96-well microplates and incubated overnight. Initial experimentsindicate that FBS contains low levels of intrinsic -gal activity as evidenced by the slow conversion of Daun02to Daunomycin; however, this is not evident for human serum. Therefore, prior to addition of Daun02, theF

8、BS concentration is reduced from 10% to 1% for Panc02 cells. Human serum (10%) is used for thetransduced human cell lines. The cells are incubated for 24 h and then MTT is added. Lysis buffer (20% SDSdissolved in 50% DMF) is added 4 h after the addition of MTT and the cells are incubated overnight.

9、Theoptical density at 570 nm is determined using a BIO-RAD microplate reader. Cytotoxicity is expressed as theconcentration of drug or prodrug that produced a 50% (EC50) reduction in cell viability 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Anima

10、l Mice 3Administration 3 Male athymic BALB/c mice (nu/nu genotype, 18-20 g) are used. Daunomycin is administered at a dose of 20mg/kg in 100 L normal saline solution into the tail vein. Daun02 is administered intraperitoneallyat a dose of200 mg/kg in 200 L vehicle. (This route is selected because th

11、e volume of drug solution, 200 L, is too greatfor tail vein administration.) Tumor volume is determined bycaliper measurement in two dimensions andconverted to tumor mass. Tumor growth is monitored over a period of 30 days or until the tumors hasreached a mass of 5% of bodyweight (about 1 g). The an

12、imals are then killed bycarbon dioxide asphyxiation.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) Sci Rep. 2017 Jan 3;7:39817.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedCh

13、emE1. Koya E, et al. Targeted disruption of cocaine-activated nucleus accumbens neurons prevents context-specific sensitization. NatNeurosci. 2009 Aug;12(8):1069-73.2. Lehmann M, et al. Activity of topoisomerase inhibitors daunorubicin, idarubicin, and aclarubicin in the Drosophila Somatic Mutation andRecombination Test. Environ Mol Mutagen. 2004;43(4):250-7.3. Farquhar D, et al. Suicide gene therapy using E. coli beta-galactosidase.Cancer Chemother Pharmacol. Cancer Chemother Pharmacol.2002 Jul;50(1):65