产品描述:
Pazopanib is a potent and selective multi-targeted receptor tyrosine kinase inhibitor. It is an orally available angiogenesis inhibitor targeting vascular endothelial growth factor receptor (VEGFR), platelet-derived growth factor receptor (PDGFR) and c-kit. It inhibits the VEGF receptors VEGFR1, VEGFR2 and VEGFR3 (IC50s = 10, 30 and 47 nM, respectively, in a cell-free enzyme assay) and also inhibits PDGFR, FGFR, c-Kit and c-fms with IC50 values of 84nM, 74nM, 140nM and 146nM, respectively, all key proteins responsible for tumor growth and angiogenesis. Pazopanib is an anti-tumor and anti-angiogenic agent. It inhibits upregulation of the surface adhesion proteins ICAM-1 and VCAM-1 induced by VEGF in multiple myeloma cells co-cultured with human umbilical vein endothelial cells (HUVECs) and decreases multiple myeloma cell adhesion to HUVECs. It also inhibits proliferation of multiple myeloma cells co-cultured with HUVECs. Pazopanib reduces tumor growth, induces apoptosis, decreases angiogenesis and increases survival in vivo in multiple myeloma mouse xenograft model. Formulations containing pazopanib have been used in the treatment of cancer.