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[1].
| Animal Model: | BALB/c nude mice, female, 6–7 weeks of age with NCI-H1975 tumor xenograft[1] |
| 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[1] |
| 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 Tmax | 8 h | | Cmax | 39.4 μg/L | | AUC0-a | 780 μg/L*h | | IV | 5 mg/kg | | half life | 4.9 h | | oral bioavailability | 28.8% |
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