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hVEGF-IN-1

CAS No. : 1637443-98-1

MCE 国际站：hVEGF-IN-1

产品活性：hVEGF-IN-1，一种喹唑啉衍生物，可以特异性结合内部核糖体进入位点 A (IRES-A) 中富含 G 的序列，并会使 G-四链体结构不稳定。在 SPR 实验中，hVEGF-IN-1 以 0.928 μM 的 K_d 值与 IRES-A (WT) 结合。hVEGF-IN-1 可通过降低 VEGF-A 蛋白表达来阻止肿瘤细胞迁移并抑制肿瘤生长。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：VEGFR

In Vitro: hVEGF-IN-1 (compound 1) (1 nM-100 μM; 5 min) binds to IRES-A (WT) and IRES-A mutant RNA oligomer (IRES-MU1) with K_ds of 1.29 and 13.4 μM by microscale thermophoresis (MST) measurements, respectively.
hVEGF-IN-1 (0.375-3 μM; 0-24 h) reduces MDA-MB-231 cell migration approximately 25% at the concentration of 3 μM.
hVEGF-IN-1 (0.1875-3 μM; 48 h) reduces the level of VEGF-A protein in MCF-7 cells.
hVEGF-IN-1 (0.375-3 μM; 48 h) decreases the relative wound closure of migrated MCF-7 cells by ∼35% at the concentration of 3 μM.
hVEGF-IN-1 (1.25-10 μM) reduces the stability of the IRES-A G-Quadruplex in a dose-dependent manner.

In Vivo: hVEGF-IN-1 (compound 1) (7.5 mg/kg; i.p. once daily for 20 d) inhibits tumor growth in a human breast tumor xenograft.

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