产品
编 号：F715064
分子式：C33H27FN4O4
分子量：562.59
分子式：C33H27FN4O4
分子量：562.59
产品类型
规格
价格
是否有货
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2101241-90-9
产品详情
生物活性：
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
体内研究：
MET kinase-IN-2 (3-37.5 mg/kg; p.o.; 7 days per week for 3 weeks) exhibits statistically significant tumor growth inhibition in the U-87 MG 24 xeograft model.MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2，CL, and F% values are 1.5 μg/mL, 10.7 μg?h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively.Animal Model:4-6 weeks old Female nude mice (U-87 MG xenograft model)
Dosage:3, 6, 12.5, 37.5 mg/kg
Administration:P.o.; 7 days per week for 3 weeks
Result:Induced dose-dependent tumor growth inhibition.
Animal Model:Male SD rats
Dosage:5 mg/kg
Administration:P.o. (Pharmacokinetic Analysis)
Result:Displayed favorable overall PK profiles, with maximal plasma concentration (Cmax=1.5 μg/mL, 5-fold higher to that of IV), plasma exposure (AUC0-∞=10.7 μg?h/mL, 9.7-fold higher to that of IV), half-life (T1/2=4.9 h, 4.9-fold longer to that of IV), total clearance CL (0.5 L/h/kg; 10-fold lower to that of IV), and oral bioavailability (F=32%, 2.7-fold higher to that of IV) after oral dose of 5 mg/kg (10 mg/kg for IV).
体外研究：
MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM.MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM.
MET kinase-IN-2 is a potent, selective, orally bioavailable MET kinase inhibitor with an IC50 of 7.4 nM. MET kinase-IN-2 has antitumor activity.
体内研究：
MET kinase-IN-2 (3-37.5 mg/kg; p.o.; 7 days per week for 3 weeks) exhibits statistically significant tumor growth inhibition in the U-87 MG 24 xeograft model.MET kinase-IN-2 treatment shows that the Cmax, AUC0-∞, T1/2，CL, and F% values are 1.5 μg/mL, 10.7 μg?h/mL, 4.9 hours, 0.5 L/h/kg, and F=32%, respectively.Animal Model:4-6 weeks old Female nude mice (U-87 MG xenograft model)
Dosage:3, 6, 12.5, 37.5 mg/kg
Administration:P.o.; 7 days per week for 3 weeks
Result:Induced dose-dependent tumor growth inhibition.
Animal Model:Male SD rats
Dosage:5 mg/kg
Administration:P.o. (Pharmacokinetic Analysis)
Result:Displayed favorable overall PK profiles, with maximal plasma concentration (Cmax=1.5 μg/mL, 5-fold higher to that of IV), plasma exposure (AUC0-∞=10.7 μg?h/mL, 9.7-fold higher to that of IV), half-life (T1/2=4.9 h, 4.9-fold longer to that of IV), total clearance CL (0.5 L/h/kg; 10-fold lower to that of IV), and oral bioavailability (F=32%, 2.7-fold higher to that of IV) after oral dose of 5 mg/kg (10 mg/kg for IV).
体外研究：
MET kinase-IN-2 (compound 20j; 72 hours) inhibits U-87 MG, NIH-H460, HT-29, and MKN-45 cell lines with IC50s ranging 2.9 to 4.5 μM.MET kinase-IN-2 inhibits AXL, Flt4, KDR, Mer, TEK, and TYRO3 with IC50s ranging from 16.5 to 198 nM.
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