For research use only. Not for therapeutic Use.
ZM323881 hydrochloride is a potent and selective VEGFR2 inhibitor with an IC50 of less than 2 nM.
ZM323881 is an anilinoquinazoline that potently inhibits VEGFR2 (KDR) tyrosine kinase activity anddemonstrates excellent selectivity versus other receptor tyrosine kinases, including PDGFRβ, FGFR1, EGFR and erbB2 (IC50>50 μM). ZM323881 inhibits VEGF-A-induced endothelial cell proliferation(IC50=8 nM) 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 hepatocyte growth factor (HGF) receptor. In HAECs, ZM323881 completely inhibits VEGF-induced ERK phosphorylation at 1 μM[2]
| Catalog Number | I002468 |
| CAS Number | 193000-39-4 |
| Synonyms | 4-fluoro-2-methyl-5-[(7-phenylmethoxyquinazolin-4-yl)amino]phenol;hydrochloride |
| Molecular Formula | C22H19ClFN3O2 |
| Purity | ≥95% |
| InChI | InChI=1S/C22H18FN3O2.ClH/c1-14-9-18(23)20(11-21(14)27)26-22-17-8-7-16(10-19(17)24-13-25-22)28-12-15-5-3-2-4-6-15;/h2-11,13,27H,12H2,1H3,(H,24,25,26);1H |
| InChIKey | AVRHWGLIYGJSOD-UHFFFAOYSA-N |
| SMILES | CC1=CC(=C(C=C1O)NC2=NC=NC3=C2C=CC(=C3)OCC4=CC=CC=C4)F.Cl |
| Reference | [1]. Whittles CE, et al. ZM323881, a novel inhibitor of vascular endothelial growth factor-receptor-2 tyrosine kinase activity. Microcirculation. 2002 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 in human aortic endothelial cell responses to VEGF. J Recept Signal Transduct Res. 2003;23(2-3):239-54. |
