产品
编 号：F756507
分子式：C28H31ClN8O3
分子量：563.05
分子式：C28H31ClN8O3
分子量：563.05
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
结构图
CAS No: 2872588-02-6
产品详情
生物活性：
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
体内研究：
FAK-IN-2 (5 and 15 mg/kg; 16 days; once daily) has potent antitumor effects in model mice with a dose-dependent manner without significant toxicityPharmacokinetic Parameters of FAK-IN-2 in male Sprague-Dawley rats.PO (5 mg/kg) IV (5 mg/kg)
Cmax (μg/L)239.872965.27
Tmax (h)1.440.08
T1/2 (h)4.707.57
Clz (L/h/kg)9.922.19
AUC0-t (μg*h/L)512.752439.06
F %21.02%
Animal Model:Female Balb/C nu/nu mice (HCT116-injected)
Dosage:5 and 15 mg/kg
Administration:16 days; once daily
Result:Displayed potent antitumor effects in a dose-dependent manner without significant toxicity.
体外研究：
FAK-IN-2 (compound 11w) (0-5 μM; 72 hours) has high anti-proliferation activities on cancer cell lines, as well as certain toxicity on normal cell lines.FAK-IN-2 (0-30 nM; 14 days) can remarkably affect HCT-116 cells clone formation in a dose-dependent manner.FAK-IN-2 (10-500 nM; 24 and 48 hours) significantly inhibits the migration of HCT116 cells at both 24 h and 48 h in a dose-dependent manner.FAK-IN-2 (0.001-10 μM; 4 and 24 hours) inhibits the phosphorylation of FAK and its downstream proteins from multiple pathways.FAK-IN-2 (0.01-1 μM; 24 or 48 hours) induces strong cell cycle arrest at the G2/M phase and apoptosis.
FAK-IN-2 is a potent and orally active focal adhesion kinase (FAK) inhibitor, with anticancer activity (FAK IC50= 35 nM). FAK-IN-2 covalently inhibits the autophosphorylation of FAK in a dose-dependent manner, and inhibits the clone formation and migration of tumor cells, inducing apoptosis.
体内研究：
FAK-IN-2 (5 and 15 mg/kg; 16 days; once daily) has potent antitumor effects in model mice with a dose-dependent manner without significant toxicityPharmacokinetic Parameters of FAK-IN-2 in male Sprague-Dawley rats.PO (5 mg/kg) IV (5 mg/kg)
Cmax (μg/L)239.872965.27
Tmax (h)1.440.08
T1/2 (h)4.707.57
Clz (L/h/kg)9.922.19
AUC0-t (μg*h/L)512.752439.06
F %21.02%
Animal Model:Female Balb/C nu/nu mice (HCT116-injected)
Dosage:5 and 15 mg/kg
Administration:16 days; once daily
Result:Displayed potent antitumor effects in a dose-dependent manner without significant toxicity.
体外研究：
FAK-IN-2 (compound 11w) (0-5 μM; 72 hours) has high anti-proliferation activities on cancer cell lines, as well as certain toxicity on normal cell lines.FAK-IN-2 (0-30 nM; 14 days) can remarkably affect HCT-116 cells clone formation in a dose-dependent manner.FAK-IN-2 (10-500 nM; 24 and 48 hours) significantly inhibits the migration of HCT116 cells at both 24 h and 48 h in a dose-dependent manner.FAK-IN-2 (0.001-10 μM; 4 and 24 hours) inhibits the phosphorylation of FAK and its downstream proteins from multiple pathways.FAK-IN-2 (0.01-1 μM; 24 or 48 hours) induces strong cell cycle arrest at the G2/M phase and apoptosis.
产品资料
Copyright©2015-2024 沪ICP备2022026524号-1
沪公网安备