PF-573228 - FAK 抑制劑 - 生命科學試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPF-573228Cat. No.: HY-10461CAS No.: 869288-64-2分式: CHFNOS分量: 491.49作靶點: FAK作通路: Protein Tyrosine Kinase/RTK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 : 51 mg/mL (103.77 mM)H2O : 40% PEG3

2、00 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.09 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (5.09 mM); Suspended solution; Need ultrasonic1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (5.09

3、 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 PF-573228有效的和選擇性的FAK抑制劑，對FAK純化重 組催化段的IC50值為4 nM。IC50 & Target IC50: 4 nM (FAK) 1體外研究 PF-573228 inhibits purified recombinant catalytic fragment of FAK with an IC50 of 4 nM. In cultured cells, PF-573228 inhibits FAK phosphorylation on Tyr397 with an IC50 of

4、30-100 nM. Treatment of cells withconcentrations of PF-573228 that significantly decreased FAK Tyr397 phosphorylation fails to inhibit cellgrowth or induce apoptosis. In contrast, treatment with PF-573228 inhibits both chemotactic and haptotacticmigration concomitant with the inhibition of focal adh

5、esion turnover 1.PROTOCOLKinase Assay 1 Purified activated FAK kinase domain is reacted with 50 M ATP, and 10 g/well of a random peptidepolymer of Glu and Tyr (molar ratio of 4:1), poly (Glu/Tyr) in kinase buffer for 15 min. Phosphorylation ofpoly(Glu/Tyr) is challenged with sMCE has not independent

6、ly confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 REF52 or PC3 cells are seeded into a 24-well plate in triplicate 24 h prior to daily treatment with the indicatedconcentrations of each inhibitor (PF-573228) for 3 days. Subsequently, the cells are harvested and cou

7、nted.Apoptosis assays are performed using a cell death detection ELISA. REF52, PC3 or MDCKcells are treatedfor 24 h (16 h for MDCK) with the indicated concentrations of each inhibitor prior to lysis. Cells suspended for16-24 h in serum-free medium served as a positive control. The cell lysates are i

8、ncubated in duplicate in theELISA system. The data represent the meansstandard deviation of one of three experiments performed induplicate 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產品發(fā)表的科研獻 Biomaterials. 2018 Oct 15;188:130-143. Biomaterials.

9、 2018 Sep;178:281-292. Cell Adh Migr. 2017 Jul 4;11(4):327-337.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Slack-Davis JK, et al. Cellular characterization of a novel focal adhesion kinase inhibitor. J Biol Chem. 2007 May 18;282(20):14845-52.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not been fully validated for medi