AZ-PFKFB3-67
Based on 1 publication(s) in Google Scholar
AZ-PFKFB3-67 is a potent and selective PFKFB3 kinase inhibitor with IC50s of 11, 159 and 1130 nM for PFKFB3, PFKFB2 and PFKFB1, respectively. AZ-PFKFB3-67 reduces MCL-1. AZ-PFKFB3-67 has neuroprotective activity.
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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: 97.03%
- CAS 番号: 1704741-11-6
- 分子式: C26H25N5O3
- 分子量:455.51
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
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MedChemExpress（MCE）の使用を引用している文献 AZ-PFKFB3-67
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生物活性
IC50: 11 nM (PFKFB3), 159 nM (PFKFB2), 1130 nM (PFKFB1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>30 μM
Compound: 67
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Inhibition of PFKFB3 in human A549 cells assessed as decrease in lactate secretion after 4 hrs
Inhibition of PFKFB3 in human A549 cells assessed as decrease in lactate secretion after 4 hrs
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[PMID: 25849762] |
| A549 | IC50 |
0.281 μM
Compound: 67
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Inhibition of PFKFB3 in human A549 cells assessed as reduction of fructose-1,6-bisphosphate formation after 4 hrs by MS/MS analysis
Inhibition of PFKFB3 in human A549 cells assessed as reduction of fructose-1,6-bisphosphate formation after 4 hrs by MS/MS analysis
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[PMID: 25849762] |
AZ-PFKFB3-67 (25 μM;) inhibits PFKFB3 activity in cells, as shown by decreased MCL-1 protein levels in both SU-DHL-4 and OCI-LY-1 cells[2]. AZ-PFKFB3-67 (10 nM; 24 h) co-treated with Roxadustat (HY-13426) significantly reverses the enhanced cell death of Roxadustat-treated neurons exposed to oxygen-glucose deprivation[3].
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 1704741-11-6
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性状 Solid
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分子量 455.51
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分子式 C26H25N5O3
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Color White to off-white
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SMILES
O=C([C@H]1NCCC1)NC2=CC=C(OC3=CC4=C(N(CC5=C(C)ON=C5C)C=C4C#N)C=C3)C=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 In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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J Cancer
B7-H3 suppresses CD8+ T cell immunologic function through reprogramming glycolytic metabolism. [Abstract]2024 Mar 11;15(9):2505-2517. PMID: 38577598
溶剤 & 溶解度
DMSO : 100 mg/mL (219.53 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: ≥ 1 mg/mL (2.20 mM); Clear solution
This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (10.0 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% Saline
Solubility: ≥ 1 mg/mL (2.20 mM); Clear solution
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 (273 KB)
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SDS (251 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Boyd S, et al. Structure-Based Design of Potent and Selective Inhibitors of the Metabolic Kinase PFKFB3. J Med Chem. 2015;58(8):3611-3625. [Content Brief]
[2]. Sneyers F, et al. Intracellular BAPTA directly inhibits PFKFB3, thereby impeding mTORC1-driven Mcl-1 translation and killing MCL-1-addicted cancer cells. Cell Death Dis. 2023 Sep 8;14(9):600. [Content Brief]
[3]. Madai S, et al. Activation of the hypoxia-inducible factor pathway protects against acute ischemic stroke by reprogramming central carbon metabolism. Theranostics. 2024 Apr 29;14(7):2856-2880. [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 | 2.1953 mL | 10.9767 mL | 21.9534 mL | 54.8835 mL |
| 5 mM | 0.4391 mL | 2.1953 mL | 4.3907 mL | 10.9767 mL | |
| 10 mM | 0.2195 mL | 1.0977 mL | 2.1953 mL | 5.4884 mL | |
| 15 mM | 0.1464 mL | 0.7318 mL | 1.4636 mL | 3.6589 mL | |
| 20 mM | 0.1098 mL | 0.5488 mL | 1.0977 mL | 2.7442 mL | |
| 25 mM | 0.0878 mL | 0.4391 mL | 0.8781 mL | 2.1953 mL | |
| 30 mM | 0.0732 mL | 0.3659 mL | 0.7318 mL | 1.8295 mL | |
| 40 mM | 0.0549 mL | 0.2744 mL | 0.5488 mL | 1.3721 mL | |
| 50 mM | 0.0439 mL | 0.2195 mL | 0.4391 mL | 1.0977 mL | |
| 60 mM | 0.0366 mL | 0.1829 mL | 0.3659 mL | 0.9147 mL | |
| 80 mM | 0.0274 mL | 0.1372 mL | 0.2744 mL | 0.6860 mL | |
| 100 mM | 0.0220 mL | 0.1098 mL | 0.2195 mL | 0.5488 mL |
AZ-PFKFB3-67 関連分類
HY-101972 関連分類
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