产品
编 号：F196838
分子式：C34H43N7O2
分子量：581.75
分子式：C34H43N7O2
分子量：581.75
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
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5mg
询价
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10mg
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50mg
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结构图
CAS No: 1637443-98-1
产品详情
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 the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression.
体内研究：
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.Animal Model:BALB/c female nude mice were implanted MCF-7 cells
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.
体外研究：
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.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.
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 the G-quadruplex structure. hVEGF-IN-1 binds to the IRES-A (WT) with a Kd of 0.928 μM in SPR experiments. hVEGF-IN-1 could hinder tumor cells migration and repress tumor growth by decreasing VEGF-A protein expression.
体内研究：
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.Animal Model:BALB/c female nude mice were implanted MCF-7 cells
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.
体外研究：
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.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.
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