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Kd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。
| 生物活性 | hVEGF-IN-1, a quinazoline derivative, could specifically bind to the G-rich sequence in the internal ribosome entry site A (IRES-A) and destabilize theG-quadruplexstructure. hVEGF-IN-1 binds to the IRES-A (WT) with aKdof 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasingVEGF-Aprotein expression[1]. |
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体外研究
(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 Kds of 1.29 and 13.4 μM by microscale thermophoresis (MST) measurements, respectively[1].
hVEGF-IN-1 (0.375-3 μM; 0-24 h) reduces MDA-MB-231 cell migration approximately 25% at the concentration of 3 μM[1].
hVEGF-IN-1 (0.1875-3 μM; 48 h) reduces the level of VEGF-A protein in MCF-7 cells[1].
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[1].
hVEGF-IN-1 (1.25-10 μM) reduces the stability of the IRES-A G-Quadruplex in a dose-dependent manner[1].
Western Blot Analysis[1] | Cell Line: | MCF-7 cells | | Concentration: | 0.1875, 0.375, 0.75, 1.5, 3 μM | | Incubation Time: | 48 hours | | Result: | Down-regulated hVEGF-A expression. |
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体内研究
(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[1].
| Animal Model: | BALB/c female nude mice were implanted MCF-7 cells[1] | | Dosage: | 7.5 mg/kg | | Administration: | I.p. once daily for 20 days | | Result: | Reduced the tumor volume to<300 mm3.
Reduced the tumor weight around 60.1% to a final weight of 0.18 g.
Decreased the VEGF-A level in tumor tissue. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 25 mg/mL(42.97 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.7190 mL | 8.5948 mL | 17.1895 mL | | 5 mM | 0.3438 mL | 1.7190 mL | 3.4379 mL | | 10 mM | 0.1719 mL | 0.8595 mL | 1.7190 mL |
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