KAN0438757
Based on 6 publication(s) in Google Scholar
KAN0438757 is a potent and selective inhibitor of the metabolic kinase PFKFB3 with an IC50 of 0.19 μM.
For research use only. We do not sell to patients.
- Purity: 99.41%
- CAS No.: 1451255-59-6
- Formula: C21H18FNO7S
- Molecular Weight:447.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) KAN0438757
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Biological Activity
IC50: 0.19 μM (PFKFB3)[1]
KAN0438757 (72 h) inhibits cell viability of Miapaca-2, PANC1, SW620, U-266, AMO-1 (IC50: 2.75, 3.83, 7.50, 5.08, 11.53 μM respectively)[1].
KAN0438757 (10 μM, 6 h) decreases homologous recombination (HR) activity and increases ionizing radiation (IR) induced γH2AX foci level in U2OS cells[1].
KAN0438757 (50 μM, 12 h) reduces PFKFB3 protein expression in HCT-116, SW-1463 and HUVECs[2].
KAN0438757 (0-50 μM, 24 h) reduces glycolysis in HCT-116 cancer cells and HUVECs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1451255-59-6
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Appearance Solid
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Molecular Weight 447.43
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Formula C21H18FNO7S
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Color White to off-white
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SMILES
O=C(OCCO)C1=CC=C(NS(=O)(C2=CC(C3=CC(F)=CC=C3O)=CC=C2)=O)C=C1O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (6)
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Journal Impact Factor
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Most Recent
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Phytomedicine
YiQiFuMai ameliorates hypoperfusion-induced cerebral infarction by targeting the shear stress-PLBD1-glycolysis-angiogenesis axis. [Abstract]2026 Feb:151:157797. PMID: 41539098 -
J Orthop Translat
Txnip regulates glycolysis and tricarboxylic acid cycle balance to maintain bone homeostasis. [Abstract]2026 May 5:58:101095. PMID: 42125243 -
Cell Prolif
PFKFB4 facilitates palbociclib resistance in oestrogen receptor-positive breast cancer by enhancing stemness. [Abstract]2023 Jan;56(1):e13337. PMID: 36127291 -
Cancer Metab
PFKFB3-dependent redox homeostasis and DNA repair support cell survival under EGFR-TKIs in non-small cell lung carcinoma. [Abstract]2024 Dec 18;12(1):37. PMID: 39696407 -
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Oxid Med Cell Longev
Specific PFKFB3 Inhibitor Memorably Ameliorates Intervertebral Disc Degeneration via Inhibiting NF- κ B and MAPK Signaling Pathway and Reprogramming of Energy Metabolism of Nucleus Pulposus Cells. [Abstract]2022 Sep 21;2022:7548145. PMID: 36187335
Solvent & Solubility
DMSO : 130 mg/mL (290.55 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: 2.17 mg/mL (4.85 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.17 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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: ≥ 2.17 mg/mL (4.85 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 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.
Purity & Documentation
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Data Sheet (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
[1]. Gustafsson NMS, et al. Targeting PFKFB3 radiosensitizes cancer cells and suppresses homologous recombination. Nat Commun. 2018 Sep 24;9(1):3872. [Content Brief]
[2]. De Oliveira T, et al. Effects of the Novel PFKFB3 Inhibitor KAN0438757 on Colorectal Cancer Cells and Its Systemic Toxicity Evaluation In Vivo. Cancers (Basel). 2021 Feb 28;13(5):1011. [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, 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 | 2.2350 mL | 11.1749 mL | 22.3499 mL | 55.8747 mL |
| 5 mM | 0.4470 mL | 2.2350 mL | 4.4700 mL | 11.1749 mL | |
| 10 mM | 0.2235 mL | 1.1175 mL | 2.2350 mL | 5.5875 mL | |
| 15 mM | 0.1490 mL | 0.7450 mL | 1.4900 mL | 3.7250 mL | |
| 20 mM | 0.1117 mL | 0.5587 mL | 1.1175 mL | 2.7937 mL | |
| 25 mM | 0.0894 mL | 0.4470 mL | 0.8940 mL | 2.2350 mL | |
| 30 mM | 0.0745 mL | 0.3725 mL | 0.7450 mL | 1.8625 mL | |
| 40 mM | 0.0559 mL | 0.2794 mL | 0.5587 mL | 1.3969 mL | |
| 50 mM | 0.0447 mL | 0.2235 mL | 0.4470 mL | 1.1175 mL | |
| 60 mM | 0.0372 mL | 0.1862 mL | 0.3725 mL | 0.9312 mL | |
| 80 mM | 0.0279 mL | 0.1397 mL | 0.2794 mL | 0.6984 mL | |
| 100 mM | 0.0223 mL | 0.1117 mL | 0.2235 mL | 0.5587 mL |
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