货号	规格	价格	上海	北京	珠海	重庆	武汉
S83771-1mg买3赠1	99.80%	￥510.00 S83771-1mg ￥510.00 现货（买3赠1）	6 6	-	-	-	-
S83771-2mg买3赠1	99.80%	￥900.00 S83771-2mg ￥900.00 现货（买3赠1）	7 7	-	-	-	-
S83771-5mg促销	99.80%	￥1330.00 ￥1060.00 S83771-5mg ￥1060.00 现货	5 5	-	-	-	-
S83771-10mg促销	99.80%	￥1690.00 ￥1350.00 S83771-10mg ￥1350.00 现货	5 5	-	-	-	-
S83771-50mg促销	99.80%	￥4420.00 ￥3530.00 S83771-50mg ￥3530.00 现货	2 2	-	-	-	-
S83771-100mg促销	≥98%	￥5950.00 ￥4760.00 S83771-100mg ￥4760.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

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

靶点：

VEGFR

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. Western Blot Analysis 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.

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.

参考文献：

1. Wang SK, et, al. Discovery of Small Molecules for Repressing Cap-Independent Translation of Human Vascular Endothelial Growth Factor (hVEGF) as Novel Antitumor Agents. J Med Chem. 2017 Jul 13;60(13):5306-5319.

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.719 ml	8.595 ml	17.189 ml
5 mM	0.344 ml	1.719 ml	3.438 ml
10 mM	0.172 ml	0.859 ml	1.719 ml
50 mM	0.034 ml	0.172 ml	0.344 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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