VEGFR-2-IN-19 (Compound 15b) 是一种有效的VEGFR2抑制剂。VEGFR-2-IN-19 诱导细胞凋亡 (apoptosis)，增加细胞内活性氧 (reactive oxygen species) 水平。VEGFR-2-IN-19 可以用作抗癌剂。
| 生物活性 | VEGFR-2-IN-19 (Compound 15b) is a potentVEGFR2inhibitor. VEGFR-2-IN-19 induces cellapoptosisand increases intracellularreactive oxygen specieslevel. VEGFR-2-IN-19 can be used as an anticancer agent[1]. |
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体外研究
(In Vitro) | VEGFR-2-IN-19 (Compound 15b) (0-100 μM, 48 h) shows antiproliferative activity against cancer cells[1].
VEGFR-2-IN-19 (0-10 μM, 48 h) inhibits the phosphorylation of VEGFR2 and the Raf/MEK/ERK signaling pathway, induces cell apoptosis, and arrests cell cycle at G0/G1 phase in HT-29 cells[1].
VEGFR-2-IN-19 (0-10 μM, 12 h) increases intracellular reactive oxygen species level in HT-29 cells[1].
Cell Cytotoxicity Assay[1] | Cell Line: | HT-29 and A549 | | Concentration: | 0-100 μM | | Incubation Time: | 48 h | | Result: | Showed antiproliferative activity with IC50values of 3.38±1.3 μM and 0.63±0.04 μM against HT-29 and A549 cells, respectively. |
Western Blot Analysis[1] | Cell Line: | HT-29 | | Concentration: | 0, 1, 5, and 10 μM | | Incubation Time: | 48 h | | Result: | Effectively inhibited the phosphorylation of VEGFR2 in dose-dependent manner. Suppressed dose-dependently expression of c-Raf, ERK1/2, and MEK and phosphorylation of ERK1/2 (pERK1/2). Up-regulated caspase-3 and Bax expression, down-regulated Bcl-2 expression. |
Apoptosis Analysis[1] | Cell Line: | HT-29 | | Concentration: | 0, 1, 5, and 10 μM | | Incubation Time: | 48 h | | Result: | The total numbers of early and late apoptotic cells were increased significantly relative to that of untreated control cells in dose-dependent manner. |
Cell Cycle Analysis[1] | Cell Line: | HT-29 | | Concentration: | 0, 1, 5, and 10 μM | | Incubation Time: | 48 h | | Result: | Increased the population of cells in sub G1 and G0/G1 phase and decreased the population of cells in S phase. |
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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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