VEGFR-2-IN-19

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

VEGFR-2-IN-19 

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。

VEGFR-2-IN-19

VEGFR-2-IN-19 Chemical Structure

CAS No. : 2456315-41-4

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生物活性

VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent[1].

IC50 & Target

VEGFR2

 

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[1]

Cell Line: HT-29 and A549
Concentration: 0-100 µM
Incubation Time: 48 h
Result: Showed antiproliferative activity with IC50 values 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.

分子量

345.39

Formula

C21H19N3O2

CAS 号

2456315-41-4

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.

参考文献
  • [1]. Azimian F, et al. Synthesis and biological evaluation of diaryl urea derivatives designed as potential anticarcinoma agents using de novo structure-based lead optimization approach. Eur J Med Chem. 2020 Sep 1;201:112461.

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