EGFR-IN-74 (Compound 21) 是一种有效的EGFR抑制剂，对 EGFR L858R/T790M 的IC50为 138 nM。EGFR-IN-74 诱导癌细胞凋亡 (apoptosis)。
| 生物活性 | EGFR-IN-74 (Compound 21) is a potentEGFRinhibitor with anIC50of 138 nM againstEGFRL858R/T790M. EGFR-IN-74 inducescancercellapoptosis[1]. |
| IC50& Target[1] | EGFRL858R/T790M 138 nM (IC50) |
|
体外研究
(In Vitro) | EGFR-IN-74 (Compound 21) (72 h) 显示出对具有不同 EGFR 状态的细胞的抗癌活性[1]。
EGFR-IN-74 (0.01 μM; 24 and 48 h) 诱导癌细胞凋亡[1]。
EGFR-IN-74 与 EGFR 酶形成稳定的复合物，没有太多的结构重排[1]。
Cell Viability Assay[1] | Cell Line: | HCC827 (EGFR Del E746-A750), NCI–H1975 (EGFR L858R/T790 M), A549 (WT EGFR), A549 and BEAS-2B cells | | Concentration: | | | Incubation Time: | 72 h | | Result: | Inhibited cell viability with IC50s of 0.010 ± 0.02, 0.21 ± 0.99, 0.99 ± 0.11, 2.99 ± 0.21 and 85.14 ± 0.12 μM against HCC827 (EGFR Del E746-A750), NCI–H1975 (EGFR L858R/T790 M), A549 (WT EGFR), A549 and BEAS-2B cells respectively. |
Western Blot Analysis[1] | Cell Line: | HCC827 cells | | Concentration: | 0.01, 0.10 and 1.00 μM | | Incubation Time: | | | Result: | Showed an ability to phosphorylate AKT. |
Apoptosis Analysis[1] | Cell Line: | HCC827 cells | | Concentration: | 0.010 μM (IC50value) | | Incubation Time: | 24 and 48 h | | Result: | Induced early apoptosis and late apoptosis of 26.8% and 4.2% respectively, in comparison with control, with early apoptosis of 2.1% and late apoptosis of 1.1%. |
|
| 分子量 | |
| Formula | |
| 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. |
