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作靶点: PI3K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 : 83.3 mg/mL (172.52 mM)* me

2、ans soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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 Seletalisib (UCB5857)是有效选择性的PI3K抑制剂，IC50值为12 n

3、M。IC50 & Target PI3K12 nM (IC50)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 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.体内研究 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