PFK-015
Based on 3 publication(s) in Google Scholar
PFK-015, a derivative of 3PO, is a specific PFKFB3 inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. PFK-015 can be used for the research of multiple cancers such as lung cancer, stomach cancer, colon cancer and esophageal squamous cell carcinoma (ESCC).
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- Pureza: 99.48%
- No. CAS: 4382-63-2
- Fòrmula: C17H12N2O
- Peso molecular:260.29
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Almacenamiento: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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) PFK-015
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
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Cell Migration/Invasion Assay
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Cell Proliferation/Viability Assay
Actividad biológica
IC50: 110 nM (recombinant PFKFB3); IC50: 20 nM (PFKFB3 activity in cancer cells)[2]
PFK-015 inhibits tumor growth in a dose-dependent manner in esophageal cancer cell line in vitro[1].
PFK-015 (0-5 μM) increases HIF-1α mediated PD-L1 transcriptional activity[1].
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PFK-015 induces the expression of tumor PD-L1 via the phos-PFKFB3/HIF-1a axis[1].
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PFK-015 potently inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM[2].
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PFK-015 inhibits cancer cell proliferation in a panel of 17 cancer cell lines and suppresses glucose uptake in cancer cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
? ? PFK-015 (0-12.5 μM, 48 h) induces tumor PD-L1 expression[1].
? ? PFK-015 (0-12.5 μM, 48 h) can cause a downregulation of immune activity against tumor cells mediated by CD8 + T cells[1].
? ? PFK-015 enhances the efficacy of ESCC by enhancing CD8 + T-cell activity combining PD-1 mAb in immunocompetent mouse models such as C57BL/6 and hu-PBMC-NOG[1].
? PFK-015 (iv, 5 mg/kg) has a satisfactory half-life, exposure, tissue distribution and reasonable clearance[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 4382-63-2
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Appearance Solid
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Peso molecular 260.29
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Fòrmula C17H12N2O
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Color Light yellow to yellow
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SMILES
O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC=CC=C3C=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Suppression of PFKFB3-driven glycolysis restrains endothelial-to-mesenchymal transition and fibrotic response. [Abstract]2022 Sep 1;7(1):303. PMID: 36045132 -
Cell Rep
An ERK5-PFKFB3 axis regulates glycolysis and represents a therapeutic vulnerability in pediatric diffuse midline glioma. [Abstract]2023 Dec 18;43(1):113557. PMID: 38113141
PFK-015 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Dec 18;43(1):113557. [Abstract]
PFKFB3 inhibitor PFK-015 dose response of DIPG IV, SF8628, and DIPG 13p cell lines.
PFK-015 purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Dec 18;43(1):113557. [Abstract]
Cell proliferation (relative fluorescence units, RFU) for DIPG IV and SF8628 cells treated with PFK-015 (0.9, 1.2 μM) compared to vehicle control.
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Mol Cell Endocrinol
PFKFB3 promotes endometriosis cell proliferation via enhancing the protein stability of β-catenin. [Abstract]2024 Jan 1:579:112083. PMID: 37820851
PFK-015 purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2024 Jan 1:579:112083. [Abstract]
11Z and EESCs cells were co-cultured with PFK-015 for 24 h and their medium supernatants were collected to determine glucose and lactate concentrations (IC50: 11Z, 4.071 μmol/L; EESCs, 3.116 μmol/L).
PFK-015 purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2024 Jan 1:579:112083. [Abstract]
PFK-015 (0-30 μM) inhibited 11Z and EESCs cell viability in a dose-dependent manner.
PFK-015 purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2024 Jan 1:579:112083. [Abstract]
PFK-015 (24 h) suppressed the protein intracellular expression of PFKFB3.
PFK-015 purchased from MedChemExpress. Usage Cited in: Mol Cell Endocrinol. 2024 Jan 1:579:112083. [Abstract]
11Z and EESCs cells were plated in 6-well plates, and PFK-015 was added to the experimental group and cultured for 10–14 days to observe the colony formation.
Solvente y solubilidad
DMSO : 25.2 mg/mL (96.82 mM; Need ultrasonic and warming; 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 mg/mL (7.68 mM); Clear solution
This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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: 2 mg/mL (7.68 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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.
Pureza y Documentación
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Ficha de datos (274 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 | 3.8419 mL | 19.2093 mL | 38.4187 mL | 96.0467 mL |
| 5 mM | 0.7684 mL | 3.8419 mL | 7.6837 mL | 19.2093 mL | |
| 10 mM | 0.3842 mL | 1.9209 mL | 3.8419 mL | 9.6047 mL | |
| 15 mM | 0.2561 mL | 1.2806 mL | 2.5612 mL | 6.4031 mL | |
| 20 mM | 0.1921 mL | 0.9605 mL | 1.9209 mL | 4.8023 mL | |
| 25 mM | 0.1537 mL | 0.7684 mL | 1.5367 mL | 3.8419 mL | |
| 30 mM | 0.1281 mL | 0.6403 mL | 1.2806 mL | 3.2016 mL | |
| 40 mM | 0.0960 mL | 0.4802 mL | 0.9605 mL | 2.4012 mL | |
| 50 mM | 0.0768 mL | 0.3842 mL | 0.7684 mL | 1.9209 mL | |
| 60 mM | 0.0640 mL | 0.3202 mL | 0.6403 mL | 1.6008 mL | |
| 80 mM | 0.0480 mL | 0.2401 mL | 0.4802 mL | 1.2006 mL |
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