Phthalazine
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Phthalazine is a chemical scaffold. Phthalazine derivatives act as VEGFR-2 inhibitors, PARP-1 inhibitors, and anticancer agents. The complex of phthalazine with silver exhibits broad-spectrum antibacterial and antifungal activities against Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa PAO1, and Candida albicans. Phthalazine derivatives possess potent vasodilatory activity. Phthalazine can be used in research related to colon adenocarcinoma, breast cancer, hypertension, diabetes, and microbial infections.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 99.98%
- CAS 番号: 253-52-1
- 分子式: C8H6N2
- 分子量:130.15
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
Phthalazine-based compounds 53 and 54 potently inhibit human PARP-1 with IC50 values of 0.77 μM and 0.097 μM, respectively, with compound 54 being more potent than Olaparib (HY-10162)[2].
Phthalazine-silver complex 70 exhibits broad-spectrum antibacterial and antifungal activity against Staphylococcus aureus, Enterococcus faecalis, Escherichia coli, Pseudomonas aeruginosa PAO1, and Candida albicans, with enhanced potency against Pseudomonas aeruginosa PAO1 relative to its biofilm inhibition activity[2].
Phthalazine derivatives 77a, 77b, 77c, 77e, 77f, and 77g exhibit potent vasorelaxant activity with IC50 values ranging from 0.10 to 0.45 μg/mL[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 253-52-1
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性状 Solid
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分子量 130.15
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分子式 C8H6N2
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Color Yellow to brown
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SMILES
C12=CC=CC=C1C=NN=C2
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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 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (768.34 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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: ≥ 5 mg/mL (38.42 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (38.42 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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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データシート (277 KB)
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SDS (418 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. El-Helby AA, et al. Design, Synthesis, Molecular Docking, and Anticancer Activity of Phthalazine Derivatives as VEGFR-2 Inhibitors. Arch Pharm (Weinheim). 2017 Dec;350(12). [Content Brief]
[2]. Sangshetti J, et al. Synthesis and biological activity of structurally diverse phthalazine derivatives: A systematic review. Bioorganic & medicinal chemistry. 2019 Sep 15;27(18):3979-3997. [Content Brief]
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 7.6834 mL | 38.4172 mL | 76.8344 mL | 192.0861 mL |
| 5 mM | 1.5367 mL | 7.6834 mL | 15.3669 mL | 38.4172 mL | |
| 10 mM | 0.7683 mL | 3.8417 mL | 7.6834 mL | 19.2086 mL | |
| 15 mM | 0.5122 mL | 2.5611 mL | 5.1223 mL | 12.8057 mL | |
| 20 mM | 0.3842 mL | 1.9209 mL | 3.8417 mL | 9.6043 mL | |
| 25 mM | 0.3073 mL | 1.5367 mL | 3.0734 mL | 7.6834 mL | |
| 30 mM | 0.2561 mL | 1.2806 mL | 2.5611 mL | 6.4029 mL | |
| 40 mM | 0.1921 mL | 0.9604 mL | 1.9209 mL | 4.8022 mL | |
| 50 mM | 0.1537 mL | 0.7683 mL | 1.5367 mL | 3.8417 mL | |
| 60 mM | 0.1281 mL | 0.6403 mL | 1.2806 mL | 3.2014 mL | |
| 80 mM | 0.0960 mL | 0.4802 mL | 0.9604 mL | 2.4011 mL | |
| 100 mM | 0.0768 mL | 0.3842 mL | 0.7683 mL | 1.9209 mL |
Phthalazine 関連分類
HY-W002016 関連分類
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