产品
编 号：F747682
分子式：C30H33ClN6O4
分子量：577.07
分子式：C30H33ClN6O4
分子量：577.07
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CAS No: 1879071-97-2
产品详情
生物活性：
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research.
体内研究：
EGFR/HER2-IN-5 (compound 6h) (oral gavage; 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg; every other day or every day;25 days) has good cancer suppression effect in a dose-dependent manner in the constructed NCI-H1975 tumor xenograft model.Animal Model:BALB/c nude mice, female, 6–7 weeks of age with NCI-H1975 tumor xenograft
Dosage:99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg
Administration:Oral gavage; 99.5 mg/kg and 24.9 mg/kg for every other day for 25 days;6.2 mg/kg for every day for 25 days
Result:Inhibited 84.11% of tumor xenografts growth at 99.5 mg/kg, 65.72% at 24.9 mg/kg, and 47% at 6.2 mg/kg in nude mice.
Animal Model:BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg; 25 days
Result:The pharmacokinetic parameters of EGFR/HER2-IN-5 (compound 6h) oral (10 mg/kg)Parameter
Oral Tmax8 h
Cmax39.4 μg/L
AUC0-a780 μg/L*h
IV5 mg/kg
half life4.9 h
oral bioavailability28.8%
体外研究：
EGFR/HER2-IN-5 (compound 6h) (0-10 μM, 72 hours) shows good anti-proliferative activity against lung cancer, where the effect against mutant lung cancer HCC 827 is superior to that of NCI-H1975 and A431.
EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research.
体内研究：
EGFR/HER2-IN-5 (compound 6h) (oral gavage; 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg; every other day or every day;25 days) has good cancer suppression effect in a dose-dependent manner in the constructed NCI-H1975 tumor xenograft model.Animal Model:BALB/c nude mice, female, 6–7 weeks of age with NCI-H1975 tumor xenograft
Dosage:99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg
Administration:Oral gavage; 99.5 mg/kg and 24.9 mg/kg for every other day for 25 days;6.2 mg/kg for every day for 25 days
Result:Inhibited 84.11% of tumor xenografts growth at 99.5 mg/kg, 65.72% at 24.9 mg/kg, and 47% at 6.2 mg/kg in nude mice.
Animal Model:BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg; 25 days
Result:The pharmacokinetic parameters of EGFR/HER2-IN-5 (compound 6h) oral (10 mg/kg)Parameter
Oral Tmax8 h
Cmax39.4 μg/L
AUC0-a780 μg/L*h
IV5 mg/kg
half life4.9 h
oral bioavailability28.8%
体外研究：
EGFR/HER2-IN-5 (compound 6h) (0-10 μM, 72 hours) shows good anti-proliferative activity against lung cancer, where the effect against mutant lung cancer HCC 827 is superior to that of NCI-H1975 and A431.
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