EGFR kinase inhibitor 1 是一种有效的EGFR抑制剂，对 WT, l885R/T790M, L858R/T790M/C797S 的IC50分别为 37、1.7、>300 nM。EGFR kinase inhibitor 1 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。EGFR kinase inhibitor 1 抑制细胞转移。EGFR kinase inhibitor 1 具有抗增殖和抗肿瘤活性。
| 生物活性 | EGFRkinase inhibitor 1 is a potentEGFRinhibitor withIC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively.EGFRkinase inhibitor 1 inducesapoptosisand cell cycle arrest at G0/G1-phase.EGFRkinase inhibitor 1 inhibits the cell motility.EGFRkinase inhibitor 1 shows antiproliferative and anti-tumor activity[1]. |
| IC50& Target[1] | EGFR (WT) 37 nM (IC50) | EGFRL858R/T790M 1.7 nM (IC50) | EGFRL858R/T790M/C797S >300 nM (IC50) |
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体外研究
(In Vitro) | EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity withIC50s of 4.17, 0.052 μM for A549, H1975 cells, respectively[1].
EGFR kinase inhibitor 1 (0.05, 0.5, 5 μM; 48 h) induces apoptosis in a dose-dependent manner[1].
EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase[1].
EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells[1].
Cell Cytotoxicity Assay[1]| Cell Line: | A549, H1975 cells | | Concentration: | | | Incubation Time: | 72 h | | Result: | Showed antiproliferation activity withIC50s of 4.17, 0.052 μM for A549, H1975 cells, respectively. |
Apoptosis Analysis[1]| Cell Line: | H1975 cells | | Concentration: | 0.05, 0.5, 5 μM | | Incubation Time: | 48 h | | Result: | Induced apoptosis in a dose-dependent manner. |
Apoptosis Analysis[1]| Cell Line: | H1975 cells | | Concentration: | 4, 20, 100 nM | | Incubation Time: | 48 h | | Result: | Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM. |
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| 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. |
