ZM323881
| 中文名称 | ZM323881 |
|---|---|
| 中文同义词 | 4-氟-2-甲基-5-[[7-(苯基甲氧基)-4-喹唑啉基]氨基]苯酚;化合物 T21540 |
| 英文名称 | 5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL |
| 英文同义词 | 5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL;KDR/FLK-1 INHIBITOR V;VEGF RECEPTOR 2 KINASE INHIBITOR V;ZM323881;4-Fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]phenol;CS-744;Phenol, 4-fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]- |
| CAS号 | 193001-14-8 |
| 分子式 | C22H18FN3O2 |
| 分子量 | 375.4 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | Mol File |
| 结构式 |  |
ZM323881 性质
| 沸点 | 543.6±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.342±0.06 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | 溶于二甲基亚砜 |
| 形态 | 白色至类白色固体。 |
| 酸度系数(pKa) | 9.99±0.23(Predicted) |
ZM323881是有效，选择性的 VEGFR2 抑制剂， IC50 值小于2 nM。
|
VEGFR2 2 nM (IC 50 ) |
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 (IC 50 >50 μM). ZM323881 inhibits VEGF-A-induced endothelial cell proliferation(IC 50 =8 nM) and VEGFR2 tyrosine phosphorylation. 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.