VEGFR2-IN-1

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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。

VEGFR2-IN-1 

VEGFR2-IN-1 是一种有效的选择性 VEGFR2 抑制剂 (IC50=19.8 nM)。VEGFR2-IN-1 通过凋亡激活和抑制 VEGFR2 的表达来抑制细胞的增殖和迁移。

VEGFR2-IN-1

VEGFR2-IN-1 Chemical Structure

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生物活性

VEGFR2-IN-1 is a potent and selective VEGFR2 inhibitor (IC50=19.8 nM). VEGFR2-IN-1 inhibits cell proliferation and migration through apoptosis activation and VEGFR2 inhibition[1].

IC50 & Target

VEGFR2

19.8 nM (IC50)

体外研究
(In Vitro)

VEGFR2-IN-1 (compound 17; 0.1, 1, 10, 100 μM; 48 hours) shows an effective and selective agent against MCF-7 (IC50=1.18 μM), MDA-MB-231 (IC50=10.49 μM), MCF-10A (IC50=24.76 μM) cells[1]. VEGFR2-IN-1 (MCF-7 cells; 48 hours) induces cell cycle arrest at the G1 and S-phases[1]. VEGFR2-IN-1 (MCF-7 cells) shows the upregulation of pro-apoptotic genes (p53, Bax, caspases-3, caspases-9) and downregulation of antiapoptotic gene (Bcl-2)[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: MCF-7, MDA-MB-231, MCF-10A cells
Concentration: 0.1, 1, 10, 100 μM
Incubation Time: 48 hours
Result: Exhibited an effective and selective agent against MCF-7 (IC50=1.18 μM), MDA-MB-231 (IC50=10.49 μM), MCF-10A (IC50=24.76 μM) cells.

体内研究
(In Vivo)

VEGFR2-IN-1 (4.2 mg/kg; i.p.; once a day for 7 days) shows anticancer activity with an improvement of hematological, biochemical parameters[1]. Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model)[1].

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

Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model)[1]
Dosage: 4.2 mg/kg
Administration: i.p.; once a days; 7 days
Result: Showed anticancer activity by having a tumor inhibition ratio of 54.2% with an improvement of hematological, biochemical parameters.

分子量

398.48

Formula

C22H18N6S
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]. Nafie MS, Boraei ATA. Exploration of novel VEGFR2 tyrosine kinase inhibitors via design and synthesis of new alkylated indolyl-triazole Schiff bases for targeting breast cancer. Bioorg Chem. 2022; 122:105708.

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