KDU691 - PI4K 抑制剂 - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEKDU691Cat. No.: HY-12912CAS No.: 1513879-19-0分式: CHClNO分量: 419.86作靶点: PI4K作通路: PI3K/Akt/mTOR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 DMSO : 150 mg/mL (357.26 mM; Need ultrasonic and warming

2、)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3817 mL 11.9087 mL 23.8175 mL5 mM 0.4763 mL 2.3817 mL 4.7635 mL10 mM 0.2382 mL 1.1909 mL 2.3817 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

3、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 (5.95 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 (5.95 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.95 mM); Clear sol

4、ution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 KDU691个 PI4K 抑制剂。IC50 & Target PI4K体内研究 During the 5 days of dosing, no major weight changes are observed in the animals that receive KDU691 asprophylactic treatment (group 691-proph). From the fourth day of dosing, the ani

5、mals that are treated withKDU691 show a transient yellow skin color. The KDU691 radical-cure group (group 691-RC) becomes blood-stage positive again at 31.80.5 days p.i. (range, 31 to 32 days). Clinical chemistry analysis of the group 691-RC monkeys reveals that bilirubin levels accumulate during th

6、e 5-day radical-cure treatment with KDU6911.PROTOCOLAnimal For in vivo PK studies, female CD-1 mice (25 to 30g) are used and randomly assigned to cages. Mice areAdministration 1 allowed to acclimate before initiation of the experiments. Feed and water are given ad libitum. KDU691 isformulated at con

7、centrations of 2.5 mg/mL and 0.25 mg/mL for a dose of 25 mg/kg and 2.5 mg/kg,respectively. The suspension formulation for p.o. dosing contains 0.5% Methyl cellulose and 0.5% Tween 80in water. After oral dosing, blood and liver samples from mice are collected at 0.08 to 24 h post dosing.Groups of thr

8、ee mice are used for each time point. Blood is centrifuged at 13,000 rpm for 7 min at 4C,plasma harvested and stored at -20C until analysis. Liver tissue samples are excised, dipped in PBS, gentlyblotted with absorbent paper, dried, weighed and stored at -20C until further analysis 1.MCE has not ind

9、ependently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Zeeman AM, et al. PI4 Kinase Is a Prophylactic but Not Radical Curative Target in Plasmodium vivax-Type Malaria Parasites.Antimicrob Agents Chemother. 2016 Apr 22;60(5):2858-63.McePdfHeightCaution: Product has not been fully validated for medica