产品
编 号：F747681
分子式：C24H27ClFN5O3
分子量：487.95
分子式：C24H27ClFN5O3
分子量：487.95
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CAS No: 1879071-89-2
产品详情
生物活性：
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research.
体内研究：
EGFR/HER2-IN-4 (compound 6d) (orally gavage; 5.1-81.4 mg/kg; for 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:81.4mg/kg, 20.4mg/kg, 5.1mg/kg
Administration:Oral gavage; 81.4mg/kg and 20.4mg/kg for every other day for 25 days; 5.1mg/kg for every day for 25 days
Result:Inhibited 95.21% of tumor xenografts growth at 81.4mg/kg, 71.01% at 20.4 mg/kg, and 55.1% at 5.1 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-4 oral (10 mg/kg) Parameter
Oral Tmax4 h
Cmax92.32 μg/L
AUC0-a1030.9 μg/L*h
IV5 mg/kg
half life6.8 h
oral bioavailability 46.1%
体外研究：
EGFR/HER2-IN-4 (compound 6d) (0-10 μM, 72 hours) shows well anti-proliferative activity against human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R) and human epithelial carcinoma cell lines A431.
EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research.
体内研究：
EGFR/HER2-IN-4 (compound 6d) (orally gavage; 5.1-81.4 mg/kg; for 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:81.4mg/kg, 20.4mg/kg, 5.1mg/kg
Administration:Oral gavage; 81.4mg/kg and 20.4mg/kg for every other day for 25 days; 5.1mg/kg for every day for 25 days
Result:Inhibited 95.21% of tumor xenografts growth at 81.4mg/kg, 71.01% at 20.4 mg/kg, and 55.1% at 5.1 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-4 oral (10 mg/kg) Parameter
Oral Tmax4 h
Cmax92.32 μg/L
AUC0-a1030.9 μg/L*h
IV5 mg/kg
half life6.8 h
oral bioavailability 46.1%
体外研究：
EGFR/HER2-IN-4 (compound 6d) (0-10 μM, 72 hours) shows well anti-proliferative activity against human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R) and human epithelial carcinoma cell lines A431.
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