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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| IC50& Target |
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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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| 分子量 |
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| Formula |
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| CAS 号 |
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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