PF-06284674
Based on 1 Customer Validation
PF-06284674 (PKM2 activator 1) (Compound 8) is a PKM2 activator that can be used in cancer research.
For research use only. We do not sell to patients.
- Purity: 99.69%
- CAS No.: 1434288-24-0
- Formula: C17H14N4O
- Molecular Weight:290.32
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Huh-7 | EC50 |
70 nM
Compound: 8
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Activation of PKM2 in human Huh7 cells assessed as production of pyruvate and ATP by fluorescence assay
Activation of PKM2 in human Huh7 cells assessed as production of pyruvate and ATP by fluorescence assay
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[PMID: 23622982] |
PF-06284674 (PKM2 activator 1) (Compound 8) activates PKM2 in Huh7 cells (EC50= 70 nM) and induces the formation of PKM2 tetramers[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1434288-24-0
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Appearance Solid
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Molecular Weight 290.32
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Formula C17H14N4O
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Color White to off-white
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SMILES
O=C1C=C(CN2C3=CC=CC=C3N=C2)N=C4N1C(C)=CC=C4
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Synonyms
PKM2 activator 1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
DMSO : 20 mg/mL (68.89 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 (stored under nitrogen). 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 (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (6.89 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 (6.89 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 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. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
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 (274 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
References
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 (stored under nitrogen). 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 | 3.4445 mL | 17.2224 mL | 34.4447 mL | 86.1119 mL |
| 5 mM | 0.6889 mL | 3.4445 mL | 6.8889 mL | 17.2224 mL | |
| 10 mM | 0.3444 mL | 1.7222 mL | 3.4445 mL | 8.6112 mL | |
| 15 mM | 0.2296 mL | 1.1482 mL | 2.2963 mL | 5.7408 mL | |
| 20 mM | 0.1722 mL | 0.8611 mL | 1.7222 mL | 4.3056 mL | |
| 25 mM | 0.1378 mL | 0.6889 mL | 1.3778 mL | 3.4445 mL | |
| 30 mM | 0.1148 mL | 0.5741 mL | 1.1482 mL | 2.8704 mL | |
| 40 mM | 0.0861 mL | 0.4306 mL | 0.8611 mL | 2.1528 mL | |
| 50 mM | 0.0689 mL | 0.3444 mL | 0.6889 mL | 1.7222 mL | |
| 60 mM | 0.0574 mL | 0.2870 mL | 0.5741 mL | 1.4352 mL |