您好,欢迎来到试剂信息网! [登录] [免费注册]
试剂信息网
位置:首页 > 产品库 > EGFR-IN-60
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
EGFR-IN-60
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-IN-60图片
CAS NO:2699877-43-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品介绍
EGFR-IN-60 (Compound 7d) 显著抑制EGFRWTEGFRT790MEGFRL858RJAK3IC50分别为 83、26、53 和 69 nM。EGFR-IN-60 抑制携带 EGFRT790M突变的 H1975 细胞和过表达 EGFRWT的 A431 细胞,IC50分别为 1.32 μM 和4.96 μM。EGFR-IN-60 具有良好的口服吸收、有效且安全的抗肿瘤活性。EGFR-IN-60 通过增加 Bax/Bcl-2 比率来诱导细胞凋亡诱导从而导致细胞死亡。
生物活性

EGFR-IN-60 (Compound 7d) shows obvious inhibition ofEGFRWT,EGFRT790M,EGFRL858RandJAK3withIC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboringEGFRT790Mmutation (IC50=1.32 μM) over A431 cells overexpressingEGFRWT(IC50=4.96 μM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death throughapoptosissupported by increased Bax/Bcl-2 ratio[1].

IC50& Target

EGFR

0.083 μM (IC50)

EGFRL858R

0.053 μM (IC50)

EGFRT790M

0.026 μM (IC50)

JAK3

0.069 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-60 (compound 7d) (3.25-88.46 μM, 48 hours) shows well antitumor activity against hepatocellular (HepG2), colorectal (HCT-116) and breast (MCF-7) cancer cells[1].
EGFR-IN-60 (compound 7d) (0.49-86.4 μM, 48 hours) shows cytotoxic activity against cancer cells[1].
EGFR-IN-60 (compound 7d) (0-5.27 μM, 24 hours) induces an increase in G2/M phase cells and induces apoptosis in HepG2, HCT-116, and MCF-7 cell lines[1].
EGFR-IN-60 (compound 7d) (0 μM, 10 μM, 24 hours) can induce apoptosis through up-regulation of Bax and down-regulation of Bcl-2[1].

Cell Proliferation Assay[1]

Cell Line:Hepatocellular (HepG2), Colorectal (HCT-116), Breast (MCF-7) cancer cells
Concentration:3.25-88.46 μM
Incubation Time:48 hours
Result:Inhibited HepG2 cells, HCT-116 cells, MCF-7 cells with IC50values of 4.46 μM, 5.27 μM and 3.25 μM respectively.

Cell Cytotoxicity Assay[1]

Cell Line:Overexpress EGFRWThuman epidermoid carcinoma cells (A431), Mutant EGFRT790Mcells NSCLC (H1975), Lung fibroblast cells (WI38), Amnion epithelial cells (WISH)
Concentration:0.49-86.4 μM
Incubation Time:48 hours
Result:Showed cytotoxic activity against A431, H1975, WI38, WISH with IC50value of 4.96 μM, 1.32 μM, 64.27 μM, 46.38 μM respectively.

Cell Cycle Analysis[1]

Cell Line:HepG2, HCT-116, MCF-7
Concentration:0 μM, 3.25 μM, 4.46 μM, 5.27 μM
Incubation Time:24 hours
Result:Resulted in an increase in the percentage of G2/M phase cells from 14.09% to 25.66% , from 15.87% to 38.51%, from 10.95% to 41.60% in HepG2, HCT-116, MCF-7 cell lines respectively.

Apoptosis Analysis[1]

Cell Line:HepG2, HCT-116, MCF-7
Concentration:3.25 μM, 4.46 μM, 5.27 μM
Incubation Time:24 hours
Result:Induced more apoptosis in MCF-7 cells comparing with HepG2 and HCT-116 cells.

Western Blot Analysis[1]

Cell Line:HepG2, HCT-116, MCF-7
Concentration:0 μM, 10 μM
Incubation Time:24 hours
Result:Showed the levels of pro-apoptotic protein Bax upgrading by 5.71, 8.15 and 16.51 fold and the levels of anti-apoptotic protein Bcl-2 down-regulating by 0.72, 0.53 and 0.31 fold in HepG2, HCT-116, MCF-7, respectively.
分子量

535.47

Formula

C28H28Cl2N6O

CAS 号

2699877-43-3

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.