Pazopanib HCl (GW786034 HCl) (C09-1016-758)

InformationPazopanib HCl (GW786034 HCl) is a novel multi-target inhibitor ofVEGFR1,VEGFR2,VEGFR3, PDGFR, FGFR, c-Kit and c-Fms withIC50of 10 nM, 30 nM, 47 nM, 84 nM, 74 nM, 140 nM and 146 nM in cell-free assays, respectively. Pazopanib induces autophagic Type II celIn vitroPazopanib potently inhibits VEGF-induced phosphorylation of VEGFR2 in HUVEC cells with IC50 of 8 nM. Pazopanib shows dose-dependent growth inhibition in all synovial sarcoma cell lines including SYO-1 and HS-SY-II cells. Proliferation of SYO-1 and HS-SY-II cells is inhibited even at 1/u2009µg/mL of Pazopanib and is completely abolished at 5/u2009µg/mL. Pazopanib induces G1 arrest, and thereby suppresses the growth of synovial sarcoma cells. Phosphorylation of Akts, GSK-3β, JNKs, p70 S6 Kinase, and mTOR is suppressed in Pazopanib-treated SYO-1 cells compared with that in the vehicle-treated cells. Pazopanib between 20 m g/mL and 22.5 m g/mL shows an increasing reduction of RPE cell viability.In vivoThe mice treated with 30 mg/kg or 100/u2009mg/kg Pazopanib reveals a significant decrease in tumor burden compared with the mice treated with vehicle or 10/u2009mg/kg Pazopanib. Treatment with Pazopanib is well-tolerated and there is no significant difference in the body weight among the mice in each group.Cell Datacell lines：Concentrations：0-10 μMIncubation Time：1 hourPowder Purity:≥99%. Specifications and Purity: 10mM in DMSO. Molecular Formula: C21H23N7O2S·HCl. Molecular Weight: 473.98.