hVEGF-IN-1
Based on 1 Customer Validation
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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.25%
- CAS 番号: 1637443-98-1
- 分子式: C34H43N7O2
- 分子量:581.75
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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生物活性
製品説明
IC50 & Target
VEGFR[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
12.5 μM
Compound: 1
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Cytotoxicity against human MCF7 cells assessed as reduction in cell viability
Cytotoxicity against human MCF7 cells assessed as reduction in cell viability
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[PMID: 28530833] |
体外実験
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 cells
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Concentration:0.1875, 0.375, 0.75, 1.5, 3 μM
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Incubation Time:48 hours
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Result:Down-regulated hVEGF-A expression.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c female nude mice were implanted MCF-7 cells[1]
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Dosage:7.5 mg/kg
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Administration:I.p. once daily for 20 days
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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.
化学情報
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CAS 番号 1637443-98-1
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性状 Solid
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分子量 581.75
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分子式 C34H43N7O2
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Color White to off-white
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SMILES
CCN(CC)CCOC(C=C1)=CC=C1NC2=NC(C3=C(NC(CCN4CCN(C)CC4)=O)C=CC=C3)=NC5=CC=CC=C52
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
溶剤 & 溶解度
体外:
DMSO : 25 mg/mL (42.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.30 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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取扱説明書 (2659 KB)
参考文献
ホットトピック
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All
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Topics
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Most Recent
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Oldest
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Topics G-quadruplex & DNA Replication
G-quadruplexes (G4s) are noncanonical nucleic acid secondary structures formed by guanine-rich sequences through stacked G-tetrads stabilized by Hoogsteen hydrogen bonding.
2026-06-18
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7190 mL | 8.5948 mL | 17.1895 mL | 42.9738 mL |
| 5 mM | 0.3438 mL | 1.7190 mL | 3.4379 mL | 8.5948 mL | |
| 10 mM | 0.1719 mL | 0.8595 mL | 1.7190 mL | 4.2974 mL | |
| 15 mM | 0.1146 mL | 0.5730 mL | 1.1460 mL | 2.8649 mL | |
| 20 mM | 0.0859 mL | 0.4297 mL | 0.8595 mL | 2.1487 mL | |
| 25 mM | 0.0688 mL | 0.3438 mL | 0.6876 mL | 1.7190 mL | |
| 30 mM | 0.0573 mL | 0.2865 mL | 0.5730 mL | 1.4325 mL | |
| 40 mM | 0.0430 mL | 0.2149 mL | 0.4297 mL | 1.0743 mL |
hVEGF-IN-1 関連分類
HY-101931 関連分類
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