EGFR-IN-7 is a potent, selective and orally active EGFR kinase inhibitor. EGFR-IN-7 has inhibitory effect for for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) with IC50 values of 7.92 nM and 0.218 nM, respectively. EGFR-IN-7 can be used for the research of various cancers[1].
EGFR-IN-7 (compound 34; 5-45 mg/kg; p.o.; daily; for 13 days) shows potent anti-tumor activity in a subcutaneously implanted Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mouse resistance model[1].
EGFR-IN-7 (25 and 50 mg/kg; p.o.; daily, for 3 weeks) has a significant inhibitory effect on tumor growth in the mouse subcutaneous xenograft PC-9 (Δ19del) model[1].
| Animal Model: | Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)[1] |
| Dosage: | 5, 15, 45 mg/kg |
| Administration: | Oral administration, daily, for 13 days |
| Result: | Significantly increased the half-life, the amount of exposure in plasma and tissues, had good pharmacokinetic effects in mice. |
| Animal Model: | Subcutaneous xenograft PC-9 (Δ19del) model[1] |
| Dosage: | 0-9 days: 50 mg/kg, 10-21 days: 25 mg/kg |
| Administration: | Oral administration, once a day, 3 weeks |
| Result: | Had a significant inhibitory effect on tumor growth, had a tumor-reducing effect and showed good antitumor efficacy. |
EGFR (WT): 7.92 nM (IC50); EGFR (C797S/T790M/L858R): 0.218 nM (IC50)
[1] Ling WY, et, al. Prostaglandin E2 suppresses bacterial killing in alveolar macrophages by inhibiting NADPH oxidase. WO2019015655A1.
