1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEZM323881 hydrochlorideCat. No.: HY-15467ACAS No.: 193000-39-4分式: CHClFNO分量: 411.86作靶點: VEGFR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 : 50 mg/mL (121.40

2、mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.07 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.07 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 ZM323881 hydrochloride有效，選擇性的 VEGFR2 抑制劑， IC50 值于2 nM。IC5

3、0 & Target VEGFR22 nM (IC50)體外研究 ZM323881 is an anilinoquinazoline that potently inhibits VEGFR2 (KDR) tyrosine kinase activityanddemonstrates excellent selectivity versus other receptor tyrosine kinases, including PDGFR, FGFR1,EGFR and erbB2 (IC5050 M). ZM323881 inhibits VEGF-A-induced endothelial

4、cell proliferation(IC50=8nM) and VEGFR2 tyrosine phosphorylation 1. ZM323881 inhibits activation of VEGFR-2, but not of VEGFR-1, epidermal growth factor receptor (EGFR), platelet-derived growth factor receptor (PDGFR), or hepatocytegrowth factor (HGF) receptor. In HAECs, ZM323881 completely inhibits

5、 VEGF-induced ERK phosphorylationat 1 M 2PROTOCOLKinase Assay 1 Compounds (ZM323881) are incubated (20 minutes, room temperature) with enzyme in an N-2-hydroxyethylpiperazine-N-2-ethanesulphonate (HEPES) (pH 7.5) buffered solution containing 10 mM MnCl2and 2 M ATP, in96-well plates coated with a pol

6、y(Glu, Ala, Tyr) 6:3:1 random copolymer substrate.Phosphorylated tyrosine is then detected bysequential incubation with mouse IgG anti-phosphotyrosineantibody a horseradish peroxidase(HRP)-linked sheep anti-mouse Ig antibody and 2,2-azino-bis(3-ethylbenzthiazoline-6-sulphonic acid). IC50 data are in

7、terpolated by nonlin-ear regression 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Cell Assay 1 HUVEC cells isolated from umbilical cords are plated (at passage 28) in 96-wellplates (1000 cells/well) anddosed with ZM323881VEGF-A (3 ng/mL), EGF (3 ng/

8、mL), or basicfibroblast growth factor (bFGF, 0.3ng/mL). The cultures are then incubated for 4 days. On day 4, the cultures are pulsed with 1 Ci/well of 3H-thymidine and reincubated for 4 hours. The cells are then harvested and assayed for the incorporation oftritium by using a beta-counter. IC50 dat

9、a are interpolated 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only. Front Physiol. 2018 Nov 30;9:1718. Oncotarget. 2016 Sep 27;7(39):63839-63855.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Whittles CE, et al. ZM323881, a nove

10、l inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE2002 Dec;9(6):513-22.2. Endo A, et al. Selective inhibition of vascular endothelial growth factor receptor-2 (VEGFR-2) identifies a central role for VEGFR-2 inhuman aortic endothelial cell responses to VEGF. J Recept Signal Transduct Res. 2003;23(2-3):239-54.McePdfHeightCaution: Product has not been full