Spebrutinib-AVL-292-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESpebrutinibCat. No.: HY-18012CAS No.: 1202757-89-8Synonyms: AVL-292; CC-292分式: CHFNO分量: 423.44作靶点: Btk作通路: Protein Tyrosine Kinase/RTK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 : 45 mg/m

2、L (106.27 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.3616 mL 11.8080 mL 23.6161 mL5 mM 0.4723 mL 2.3616 mL 4.7232 mL10 mM 0.2362 mL 1.1808 mL 2.3616 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 Spebrutinib (AVL-292; CC-292)

3、共价，选择性和服活性的 Btk 抑制剂，IC50 为0.5 nM。IC50 & Target IC50: 1体外研究Spebrutinib (CC-292) is a covalent, highly selective, orally active inhibitor of Btk with IC50 value of 0.5 nM.1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESpebrutinib also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s o

4、f 723 nM, 1.729 M, 2.43 M, 4.4 M, and 7.15 M, rspectively. Extensive analysis has revealed that the EC50 of Btk occupancy from aSpebrutinib dose-response in Ramos cells (EC50=6 nM) correlated directly with the cellular EC50 of Btkkinase inhibition with Spebrutinib (EC50=8 nM). Furthermore, the conce

5、ntration at which Spebrutinib inhibits90% of Btk activity in Ramos cells is 35 nM while the concentration of Spebrutinib required for 90%occupancy of Btk is 39 nM 1.PROTOCOLCell Assay 1 Cells are incubated in serum-free RPMI media for 1-1.5 hours. Isolated human B cells are incubated withSpebrutinib

6、 at a final concentration of 0.001, 0.01, 0.1 and 1 M. Ramos cells are incubated with 0.1 nM-3 M Spebrutinib. Cells are then incubated in the presence of compound for 1 hour at 37C. Followingincubation, cells are centrifuged and resuspended in 100 L of serum-free RPMI and BCR is stimulated withaddit

7、ion of 5 g/mL -human IgM. Samples are centrifuged, washed in phosphate-buffered saline (PBS), andlysed in 100 L of Cell Extraction Buffer plus 1:10 (v/v) PhosSTOP Phosphatase Inhibitor and 1:10 (v/v)Complete Protease Inhibitor. Antibodies used for immunoblot analysis include P-PLC2, PLC2 (3871; CST)

8、,Syk (2712; CST), P-Syk (2710; CST), Btk, P-Btk, and Tubulin. Membranes are scanned on a Li-Cor Odysseyscanner using infrared fluorescence detection 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Blood. 2016 Jun 23;127(25):3237-52. Br J P

9、harmacol. 2019 Jul 30. Stem Cell Rep. 2019 Apr. Roy Soc Open Sci. 2019 Jun. Methods Mol Biol. 2018;1711:351-398.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Evans EK, et al. Inhibition of Btk with CC-292 provides early pharmacodynamic assessment of activity in mice and humans. J PharmacolExp Ther. 2013 Aug;346(2):219-28.McePdfHeightCaution: Product has not been fully validated for med