hVEGF-IN-1 - CAS:1637443-98-1

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hVEGF-IN-1

目录号 : KM9496 CAS No. : 1637443-98-1 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
1mg		In-stock
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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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 K_d 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 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.

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 mm. Reduced the tumor weight around 60.1% to a final weight of 0.18 g. Decreased the VEGF-A level in tumor tissue.

分子量

581.75

CAS号

1637443-98-1

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

溶解性数据

In Vitro:

DMSO : 25 mg/mL (42.97 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.30 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.30 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。