VEGFR-2-IN-11

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-11 

VEGFR-2-IN-11 (Compound 8h) 是一个有效的 VEGFR-2 抑制剂,其 IC50 值为 60.27 nM。VEGFR-2-IN-11 表现出抗癌活性,诱导细胞凋亡 (apoptosis)。

VEGFR-2-IN-11

VEGFR-2-IN-11 Chemical Structure

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生物活性

VEGFR-2-IN-11 (Compound 8h) is a potent VEGFR-2 inhibitor with an IC50 of 60.27 nM. VEGFR-2-IN-11 shows antitumor activity and induces cell apoptosis[1].

IC50 & Target

VEGFR-2

60.27 nM (IC50)

体外研究
(In Vitro)

VEGFR-2-IN-11 (Compound 8h) (0-100 µM) shows antiproliferation activities against tumor cells and induces a low toxic effect in normal cells[1].
VEGFR-2-IN-11 (4.92 µM, 24h) arrests the cell cycle on MCF-7 at a G1/S phase and induces MCF-7 cell apoptosis[1].

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

Cell Proliferation Assay[1]

Cell Line: HCT-116, HEPG-2, and MCF-7
Concentration: 0-100 µM
Incubation Time:
Result: Showed antiproliferation activities with IC50 values of 8.62 ± 0.7, 10.18 ± 0.8, and 4.92 ± 0.2 µM against HCT-116, HEPG-2, and MCF-7 cells, respectively.

Cell Cycle Analysis[1]

Cell Line: MCF-7
Concentration: 4.92 µM
Incubation Time: 24 h
Result: Resulted in a significant increase in the ratio of MCF-7 cells in the G0/G1 phase from 45.81 % (untreated cells) to 49.18 % and the S phase from 39.14% (untreated cells) to 43.22% with a concomitant decrease in the number of cells in G2/M phase by 7.6% compared to untreated control (15.05%).

Apoptosis Analysis[1]

Cell Line: MCF-7
Concentration: 4.92 µM
Incubation Time: 24 h
Result: Induced the early apoptosis in MCF-7 (3.46%) 6.4 folds over the untreated cells (0.54%). Enhanced the late apoptotic induction by 20.72% compared to untreated control (0.18%). Induced total apoptosis with 36.24%.

Cell Cytotoxicity Assay[1]

Cell Line: WI-38
Concentration: 0-100 µM
Incubation Time:
Result: Induced a low toxic effect with an IC50 value of 44.45 ± 3.2 µM against WI-38 cells.

分子量

552.49

Formula

C29H22BrN5S

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]. Abdelrahman Hamdi, et al. Design, synthesis, antitumor, and VEGFR-2 inhibition activities of novel 4-anilino-2-vinyl-quinazolines: Molecular modeling studies. Bioorg Chem. 2022 May;122:105710.

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