VEGFR2-IN-1

Research use only, not for human use.

VEGFR2-IN-1 is a selective and potent VEGFR2 inhibitor with antitumor activity that inhibits cell proliferation and migration and can be used in the study of breast cancer.

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.

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.VEGFR2-IN-1 (MCF-7 cells; 48 hours) induces cell cycle arrest at the G1 and S-phases.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).Cell Cytotoxicity Assay 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.

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.Animal Model: Male Swiss albino mice, 21-28 g (Xenograft model).Animal Model:Male Swiss albino mice, 21-28 g (Xenograft model)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.

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Angiogenesis

VEGFR

VEGFR

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2765224-55-1

398.48

C22H18N6S

>98% (HPLC)

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N(=C/C=1C=2C(NC1)=CC=CC2)\N3C(=NN=C3SCC=C)C4=CC=5C(N4)=CC=CC5

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(-20℃)

With Ice Pack

≥ 2 years