EGFR-IN-45 是一种有效的表皮生长因子受体 (EGFR) 泛抑制剂，对EGFR和CDK2的IC50分别为 0.4 μM 和 1.6 μM。EGFR-IN-45 也抑制拓扑异构酶 Topo I 和 Topo II。EGFR-IN-45 能将癌细胞抑制在 G1 前期，诱导细胞凋亡 (apoptosis)。
| 生物活性 | EGFR-IN-45 is a potent epidermal growth factor receptor (EGFR) pan inhibitor, withIC50s of 0.4 μM and 1.6 μM forEGFRandCDK2, respectively. EGFR-IN-45 also inhibitTopo IandTopo II. EGFR-IN-45 arrestscancercells in the pre-G1 phase and inducesapoptosis[1]. |
| IC50& Target[1] | CDK2 1.6 μM (IC50) | EGFR 0.4 μM (IC50) |
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体外研究
(In Vitro) | EGFR-IN-45 (compound 30b) (0-10 μM; 48 hours) exhibits the high anticancer activity against Panc-1, MCF-7, HT-29 and A-549[1].
EGFR-IN-45 (20 and 100 μM; hours) can inhibit Topo I and Topo II in a dose-dependent manner[1].
EGFR-IN-45 (0-8 μM; 24 hours) has a high percentage of cell accumulation in the pre-G1 phase in MCF-7[1].
EGFR-IN-45 (0-8 μM; 24 hours) induces high amounts of apoptosis, with a necrosis percent of 2.99[1].
Cell Proliferation Assay | Cell Line: | Panc-1, MCF-7, HT-29 and A-549[1] | | Concentration: | 0-10 μM | | Incubation Time: | 48 hours | | Result: | Exhibited the high anticancer activity with IC50s of 0.9±0.20, 0.8±0.5, 1.3±0.3, 1.2±0.2 μM in Panc-1, MCF-7, HT-29 and A-549, respectively. |
Cell Cycle Analysis | Cell Line: | MCF-7[1] | | Concentration: | 0, 2, 4, 6 and 8 μM | | Incubation Time: | 24 hours | | Result: | Showed a high percentage of cell accumulation (36.02%) in the pre-G1 phase in MCF-7. |
Apoptosis Analysis | Cell Line: | MCF-7[1] | | Concentration: | 0, 2, 4, 6 and 8 μM | | Incubation Time: | 24 hours | | Result: | Induced high amounts of apoptosis, with a necrosis percent of 2.99. |
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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. |
