kok电子竞技

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPyridoclaxCat. No.: HY-12527CAS No.: 1651890-44-6Synonyms: MR-29072分式: CHN分量: 426.51作靶点: Bcl-2 Family作通路: Apoptosis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 : 20 mg/mL (46.89 mM; Need u

2、ltrasonic)H2O : 0.1 mg/mL (insoluble)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3446 mL 11.7231 mL 23.4461 mL5 mM 0.4689 mL 2.3446 mL 4.6892 mL10 mM 0.2345 mL 1.1723 mL 2.3446 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 Pyridoclax种 Mcl-1 抑制剂。IC50 & Target Mcl-1体外研究

3、Pyridoclax directly binds to Mcl-1. Without cytotoxic activity when administered as a single agent, Pyridoclax1/2 Master of Small Molecules 您边的抑制剂师www.MedChemEinduces apoptosis in combination with Bcl-xL-targeting siRNA or with ABT-737 in ovarian, lung, andmesothelioma cancer cells 1. Pyridoclax dir

4、ectly binds to Mcl-1, and hence sensitizes ovarian carcinomacells to Bcl-xL-targeting strategies. Pyridoclax induces apoptosis in ovarian, and also in lung, andmesothelioma cancer cells when it is administrated in combination with Bcl-xL-targeting siRNA or Bcl-xLtargeting molecules such as ABT-737 o

5、r its orally available derivative ABT-263 2.PROTOCOLKinase Assay 1 For donor saturating assays, Hela cells are seeded on 12-well plates and transfected with 200 ng/well ofplasmid pRluc-BimL coding for BRET donor and an increasing quantity of BRET acceptor plasmids peYFP-Mcl-1 (or with pCMV-Mcl-1 as

6、a control). Twenty-four hours after transfection, cells are trypsinized, reseededinto white flat bottom 96-well plates, and incubated for another day before measurements. A singledonor/acceptor ratio (200/800) is used to carry out the drug treatment assay. After reseeding, cells are thensubject to a

7、 16 h Pyridoclax treatment. Light emission at 485 and 530 nm is measured consecutively usingthe Mithras fluorescence-luminescence detector LB 940 after adding the luciferase substrate, coelenterazineH, at a final concentration of 5 M. BRET ratios are calculated 1.MCE has not independently confirmed

8、the accuracy of these methods. They are for reference only. Methods Mol Biol. 2018;1711:351-398.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Gloaguen C, et al. First evidence that oligopyridines, -helix foldamers, inhibit Mcl-1 and sensitize ovarian carcinoma cells to Bcl-xL

9、-targeting strategies. J Med Chem. 2015 Feb 26;58(4):1644-68.2. Groo AC, et al. Comparison of 2 strategies to enhance Pyridoclax solubility: Nanoemulsion delivery system versus salt synthesis. Eur JPharm Sci. 2017 Jan 15;97:218-226.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-820-3792;Fax:E-mail: techMedChemE2/2 Master of Small Molecules 您边的抑制剂师