193001-14-8
中文名稱
ZM323881
英文名稱
5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
CAS
193001-14-8
分子式
C22H18FN3O2
分子量
375.4
MOL 文件
193001-14-8.mol
更新日期
2025/01/19 20:16:13
193001-14-8 結(jié)構(gòu)式
基本信息
中文別名
4-氟-2-甲基-5-[[7-(苯基甲氧基)-4-喹唑啉基]氨基]苯酚 英文別名
CS-744ZM323881
KDR/FLK-1 INHIBITOR V
VEGF RECEPTOR 2 KINASE INHIBITOR V
5-((7-(BENZYLOXY)QUINAZOLIN-4-YL)AMINO)-4-FLUORO-2-METHYLPHENOL
4-Fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]phenol
Phenol, 4-fluoro-2-methyl-5-[[7-(phenylmethoxy)-4-quinazolinyl]amino]-
所屬類別
生物：小分子化合物物理化學(xué)性質(zhì)
沸點(diǎn)543.6±50.0 °C(Predicted)
密度1.342±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)9.99±0.23(Predicted)
形態(tài)白色至類白色固體
常見(jiàn)問(wèn)題列表
生物活性
ZM323881是有效，選擇性的 VEGFR2 抑制劑， IC50 值小于2 nM。靶點(diǎn)
|
VEGFR2 2 nM (IC 50 ) |
體外研究
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.