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EGFR/C797S-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
EGFR/C797S-IN-1图片
CAS NO:2378188-21-5
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
EGFR/C797S-IN-1 是一种有效的EGFR-C797S抑制剂,IC50值为 0.128 μM。EGFR/C797S-IN-1 显示出抗增殖活性和抗肿瘤活性。EGFR/C797S-IN-1 以剂量依赖的方式抑制 P-EGFR 蛋白的表达。
生物活性

EGFR/C797S-IN-1 is a potentEGFR-C797Sinhibitor with anIC50value 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[1].

IC50& Target[1]

EGFRL858R/T790M/C797S

0.128 μM (IC50)

体外研究
(In Vitro)

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[1]
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[1]

Cell Proliferation Assay[1]

Cell Line:BaF3 cells with EGFRL858R/T790M/C797S and EGFR19del/T790M/C797S Mutations
Concentration:0-10 μM
Incubation Time:72 h
Result:Showed anti-proliferative activitie with IC50s of 0.75, 0.09 μM for BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S, respectively.

Western Blot Analysis[1]

Cell Line:BaF3-EGFRL858R/T790M/C797S, BaF3-EGFR19del/T790M/C797S cells
Concentration:1, 10, 100, 1000, 10000 nM
Incubation Time:24 h
Result:Decreased the expression of p-EGFR, p-AKT. p-ERK protein in a dose dependent manner.
体内研究
(In Vivo)

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[1]

Animal Model:SD male rats[1]
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)[1]
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.
分子量

470.56

Formula

C28H30N4O3

CAS 号

2378188-21-5

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.