Seletalisib-UCB5857-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESeletalisibCat. No.: HY-16754CAS No.: 1362850-20-1Synonyms: UCB5857分式: CHClFNO分量: 482.85作靶點: PI3K作通路: PI3K/Akt/mTOR儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 83.3 mg/mL (172.52 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.0710 mL 10.3552 mL 20.7104 mL5 mM 0.4142 mL 2.0710 mL 4.1421 mL10 mM 0.2071 mL 1.0355 mL 2.0710 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Seletalisib (UCB5857)是有效選擇性的PI3K抑制劑，IC50值為12 n

3、M。IC50 & Target PI3K12 nM (IC50)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE體外研究 Seletalisib is a potent, ATP-competitive and highly selective PI3K inhibitor able to block AKTphosphorylation following activation of the BCR in a B-cell line. Seletalisib inhibits N-formyl peptides (fMLP)-stimulat

4、ed but not phorbol myristate acetate (PMA)-stimulated superoxide release from human neutrophilsconsistent with a PI3K-specific activity. No indications of cytotoxicity are observed in PBMCs or other celltypes treated with seletalisib. seletalisib blocks human T-cell production of several cytokines f

5、rom activatedT-cells. Seletalisib inhibits T-cell differentiation to Th1, Th2, and Th17 subtypes. Additionally, seletalisibinhibits B-cell proliferation and cytokine release. In human whole blood assays, seletalisib inhibits CD69expression upon B-cell activation and anti-IgE-mediated basophil degran

6、ulation 1.體內(nèi)研究 Seletalisib significantly inhibits IL-2 release following TCR stimulation in the rat. The inhibition is observed atall tested doses of seletalisib with almost complete inhibition reached at dose levels 1 mg/kg. Seletalisib haspotent in vivo effects with an estimated IC50 value of 1.PR

7、OTOCOLKinase Assay 1 Seletalisib is dissolved 1 mM solution in DMSO, and tested in a concentration response (seletalisib), toexplore the effects of PI3K-specific inhibition compared with complete inhibition of class I PI3K signaling. Inaddition, seletalisib is tested in the BioMap BT cell system at

8、concentrations of 1000, 100, 10, and 1 nM. Anactivity profile is generated based on the effect of the compounds on the levels of cellular readouts, includingcytokines, growth factors, adhesion molecules, and proliferation endpoints 1.MCE has not independently confirmed the accuracy of these methods.

9、 They are for reference only.Animal Rats: Rats are dosed with seletalisib (0.1-10 mg/kg in 500 L volume) or vehicle via oral gavage 30 min priorAdministration 1 to i.v. administration of anti- CD3 antibody administered in a 200 L dose volume. The vehicle ismethylcellulose or saline for oral and i.v.

10、 administration, respectively. Seletalisib levels and IL-2 levels aremeasured 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Allen RA, et al. Seletalisib: Characterization of a Novel, Potent, and Selective Inhibitor of PI3K. J Pharmacol Exp Ther. 2017 Apr 25. pii:jpet.116.237347.McePdfHeightCaution: Product has not been fully va