产品
编 号：F751742
分子式：C28H30N4O3
分子量：470.56
分子式：C28H30N4O3
分子量：470.56
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CAS No: 2378188-21-5
产品详情
生物活性：
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 μM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner.
体内研究：
EGFR/C797S-IN-1 (10、30 mg/kg；每日一次，持续 14 天) 呈剂量依赖性显著降低小鼠体内的肿瘤生长。Animal Model:SD male rats
Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o.
Administration:i.v. or p.o.
Result:Displayed good biochemical activity and promising cellular activity.
Animal Model:BALB/c nude mice (BaF3-EGFR19del/T790M/C797S xenograft model)
Dosage:10, 30 mg/kg
Administration:I.p.; daily for 14 days
Result:Displayed an obvious suppressive effect of tumor growth, with the TGI at 51.36% and 67.95% at the dosage of 10 mg/kg and 30 mg/kg, respectively.
体外研究：
EGFR/C797S-IN-1 (compound 14d) (0-10 μM; 72 h) 显示抗增殖活性，对BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S 的 IC50 值分别为 0.75、0.09 μM 。EGFR/C797S-IN-1 (1-10000 nM; 24 h) 以剂量依赖性降低 p-EGFR、p-AKT、p-ERK 蛋白的表达。
EGFR/C797S-IN-1 is a potent EGFR-C797S inhibitor with an IC50 value of 0.128 μM. EGFR/C797S-IN-1 shows anti-proliferative activity and anti-tumor activity. EGFR/C797S-IN-1 inhibits the expression of p-EGFR in a dose-dependent manner.
体内研究：
EGFR/C797S-IN-1 (10、30 mg/kg；每日一次，持续 14 天) 呈剂量依赖性显著降低小鼠体内的肿瘤生长。Animal Model:SD male rats
Dosage:1 mg/kg for i.v.; 10 mg/kg for p.o.
Administration:i.v. or p.o.
Result:Displayed good biochemical activity and promising cellular activity.
Animal Model:BALB/c nude mice (BaF3-EGFR19del/T790M/C797S xenograft model)
Dosage:10, 30 mg/kg
Administration:I.p.; daily for 14 days
Result:Displayed an obvious suppressive effect of tumor growth, with the TGI at 51.36% and 67.95% at the dosage of 10 mg/kg and 30 mg/kg, respectively.
体外研究：
EGFR/C797S-IN-1 (compound 14d) (0-10 μM; 72 h) 显示抗增殖活性，对BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S 的 IC50 值分别为 0.75、0.09 μM 。EGFR/C797S-IN-1 (1-10000 nM; 24 h) 以剂量依赖性降低 p-EGFR、p-AKT、p-ERK 蛋白的表达。
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