1. Protein Tyrosine Kinase/RTK
  2. VEGFR
  3. hVEGF-IN-1

hVEGF-IN-1 

目录号: HY-101931 纯度: 98.56%
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 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。

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hVEGF-IN-1 Chemical Structure

hVEGF-IN-1 Chemical Structure

CAS No. : 1637443-98-1

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5 mg ¥3900
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10 mg ¥6800
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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[1].

IC50 & Target

VEGFR[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
分子量

581.75

Formula

C34H43N7O2

CAS 号
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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
hVEGF-IN-1
目录号:
HY-101931
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