EGFR-IN-60

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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。

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EGFR^WT、EGFR^T790M、EGFR^L858R和JAK3，IC₅₀分别为 83、26、53 和 69 nM。EGFR-IN-60 抑制携带 EGFR^T790M突变的 H1975 细胞和过表达 EGFR^WT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 ofEGFR^WT,EGFR^T790M,EGFR^L858RandJAK3withIC₅₀s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboringEGFR^T790Mmutation (IC₅₀=1.32 μM) over A431 cells overexpressingEGFR^WT(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)

EGFR^L858R

0.053 μM (IC₅₀)

EGFR^T790M

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 EGFR^WThuman epidermoid carcinoma cells (A431), Mutant EGFR^T790Mcells 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.