EGFR-IN-60 (Compound 7d) 显著抑制EGFRWT、EGFRT790M、EGFRL858R和JAK3，IC50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。

EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFR WT, EGFR T790M, EGFR L858R and JAK3 with IC 50 s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFR T790M mutation (IC 50 =1.32 μM) over A431 cells overexpressing EGFR WT (IC 50 =4.96 μM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio [1].

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 IC 50 values of 4.46 μM, 5.27 μM and 3.25 μM respectively. Cell Cytotoxicity Assay [1] Cell Line: Overexpress EGFR WT human epidermoid carcinoma cells (A431), Mutant EGFR T790M cells 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 IC 50 value 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.

2699877-43-3

C28H28Cl2N6O

535.47

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years