848133-17-5
中文名稱
HKI 357
英文名稱
HKI 357
CAS
848133-17-5
分子式
C31H29ClFN5O3
分子量
574.05
MOL 文件
848133-17-5.mol
更新日期
2024/12/13 09:52:58
848133-17-5 結(jié)構(gòu)式
基本信息
中文別名
化合物HKI-357化合物 T11569
英文別名
HKI 357(2E)-N-[[4-[[(3-Chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-2-butenamide
2-Butenamide, N-[4-[[3-chloro-4-[(3-fluorophenyl)methoxy]phenyl]amino]-3-cyano-7-ethoxy-6-quinolinyl]-4-(dimethylamino)-, (2E)-
物理化學(xué)性質(zhì)
沸點(diǎn)747.6±60.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度Soluble to 100 mM in DMSO and to 25 mM in ethanol
酸度系數(shù)(pKa)12.37±0.43(Predicted)
形態(tài)粉末
顏色Off-white to yellow
常見問題列表
生物活性
HKI-357 是 EGFR 和 ERBB2 的不可逆雙重抑制劑，IC50 分別為 34 nM 和 33 nM。HKI-357 抑制 EGFR 自磷酸化 (檢測位點(diǎn)為 Y1068)，及 AKT 和 MAPK 磷酸化。靶點(diǎn)
|
EGFR 34 nM (IC 50 ) |
ErbB2 33 nM (IC 50 ) |
體外研究
HKI-357 (0.01-10 μM) is effective in suppressing ligand-induced EGFR autophosphorylation and its downstream signaling, as determined by AKT and MAPK phosphorylation in NCI-H1975 cells. HKI-357 also is effective in suppressing EGFR autophosphorylation (measured at residue Y1068), and AKT and MAPK phosphorylation in parental NCI-H1650 cells harboring the delE746-A750 EGFR mutation.
Western Blot Analysis
| Cell Line: | NCI-H1975 bronchoalveolar cell line |
| Concentration: | 0.01, 0.01, 0.1, 1 and 10 μM |
| Incubation Time: | |
| Result: | Suppressed ligand-induced EGFR autophosphorylation and its downstream signaling AKT and MAPK phosphorylation. |