EGFR-IN-49 是一种有效的选择性EGFR抑制剂，对 EGFRT790M和 EGFRT790M/L858R的IC50值分别为 65.0 nM 和 13.6 nM。EGFR-IN-49 以剂量依赖性方式诱导细胞晚期凋亡 (apoptosis)。
| 生物活性 | EGFR-IN-49 is a potent and selectiveEGFRinhibitor withIC50s of 65.0 nM and 13.6 nM forEGFRT790MandEGFRT790M/L858R, respectively. EGFR-IN-49 induces lateapoptosisin a dose-dependent manner[1]. |
| IC50& Target[1] | EGFRT790M 65.0 nM (IC50) | EGFRL858R/T790M 13.6 nM (IC50) |
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体外研究
(In Vitro) | EGFR-IN-49 (compound 13a) (1, 10 μM) shows inhibition activity for H1975 cells with an IC50of 699.2 nM[1].
EGFR-IN-49 (1 μM) shows an strong inhibitory activity to EGFRT790M, EGFRT790M/L858R, EGFRWTwith IC50s of 65.0, 13.6, >1000 nM, respectively[1].
EGFR-IN-49 (0.2, 4, 8 μM; 48 h) induces cell apoptosis in a dose-dependent manner in A431 cells[1].
Cell Proliferation Assay[1] | Cell Line: | A549, A431, Hela, MCF7, LO2 cells | | Concentration: | 0-50 μM | | Incubation Time: | | | Result: | Showed excellent anti-proliferative activities with IC50s of 4.34, 3.79, 6.39, 18.99, >50 μM for A549, A431, Hela, MCF7, LO2 cells, respectively. |
Apoptosis Analysis[1] | Cell Line: | A431 cells | | Concentration: | 0.2, 4, 8 μM | | Incubation Time: | 48 h | | Result: | Induced cell apoptosis in a low concentration (0.33 μM) and exhibited higher percent of 16.41% % in the stage of late apoptotic at concentration of 4 μM. |
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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. |
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