产品
编 号：F282636
分子式：C32H41BrN9O2P
分子量：694.6
分子式：C32H41BrN9O2P
分子量：694.6
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
50mg
询价
询价
结构图
CAS No: 2267329-76-8
产品详情
生物活性：
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.
体内研究：
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.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.Animal Model:Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)
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
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.
体外研究：
EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively.EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM.EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM.EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM.
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.
体内研究：
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.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.Animal Model:Ba/F 3 (Δ19del/T790M/C797S)-derived xenograft (CDX) BALB/c nude mice (female, 6-8 weeks, 18-22 g)
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
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.
体外研究：
EGFR-IN-7 (compound 34) (10 mM) has a strong inhibitory effect on the enzymatic activity of EGFR (WT), EGFR (Δ19del/T790M/C797S) and EGFR (C797S/T790M/L858R) with IC50 values of 7.92 nM, 0.218 nM and 0.16 nM, respectively.EGFR-IN-7 (1 mM) has excellent selectivity for EGFR (WT) in A431 cells with an IC50 value of 154 nM.EGFR-IN-7 (10 μM-0.508 nM) has a good inhibitory effect on cells of the Ba/F 3 (EGFRΔ19del/T790M/C797S) triple mutant with an IC50 value of 22 nM.EGFR-IN-7 (10 μM or 100 μM) has inhibition of phosphorylation activity of pEGFR Ba/F 3 (EGFRΔ19del/T790M/C797S) cells with an IC50 value of 19 nM.
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