GSK3182571
Based on 1 Customer Validation
GSK3182571 is a non-selective broad-spectrum kinase inhibitor with similar structure to CTx-0294885 (HY-15985). GSK3182571 can induce changes in the thermostability of target proteins in cells. GSK3182571 can be used to explore the effects of drugs on kinase networks and off-target effects in leukemia cell models.
For research use only. We do not sell to patients.
- Purity: 98.97%
- CAS No.: 2135595-04-7
- Formula: C25H31ClN8O
- Molecular Weight:495.02
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Biological Activity
GSK3182571 (20 μM; 10 min + 3 min heating) induces significant changes in the melting temperatures (Tm) of 51 kinases in a thermal proteome profiling (TPP) experiment of K562 cell extracts, which correlated with the pIC50 values[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. 2135595-04-7
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Appearance Solid
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Molecular Weight 495.02
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Formula C25H31ClN8O
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Color White to light yellow
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SMILES
O=C(NC)C1=CC=CC=C1NC2=NC(NC3=CC=C(N4CCN(CCCN)CC4)C=C3)=NC=C2Cl
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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 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (202.01 mM; ultrasonic and adjust pH to 4 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
1 M HCl : 50 mg/mL (101.01 mM; Need ultrasonic)
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.
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: ≥ 2.5 mg/mL (5.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.05 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Purity & Documentation
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Data Sheet (270 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]. Mikhail M Savitski, et al. Tracking cancer drugs in living cells by thermal profiling of the proteome. Science. 2014 Oct 3;346(6205):1255784. [Content Brief]
[2]. Mateus A, et al. Thermal proteome profiling: unbiased assessment of protein state through heat-induced stability changes. Proteome Sci. 2017 Jun 24;15:13. [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 |
|---|---|---|---|---|---|
| 1 M HCl / DMSO | 1 mM | 2.0201 mL | 10.1006 mL | 20.2012 mL | 50.5030 mL |
| 5 mM | 0.4040 mL | 2.0201 mL | 4.0402 mL | 10.1006 mL | |
| 10 mM | 0.2020 mL | 1.0101 mL | 2.0201 mL | 5.0503 mL | |
| 15 mM | 0.1347 mL | 0.6734 mL | 1.3467 mL | 3.3669 mL | |
| 20 mM | 0.1010 mL | 0.5050 mL | 1.0101 mL | 2.5252 mL | |
| 25 mM | 0.0808 mL | 0.4040 mL | 0.8080 mL | 2.0201 mL | |
| 30 mM | 0.0673 mL | 0.3367 mL | 0.6734 mL | 1.6834 mL | |
| 40 mM | 0.0505 mL | 0.2525 mL | 0.5050 mL | 1.2626 mL | |
| 50 mM | 0.0404 mL | 0.2020 mL | 0.4040 mL | 1.0101 mL | |
| 60 mM | 0.0337 mL | 0.1683 mL | 0.3367 mL | 0.8417 mL | |
| 80 mM | 0.0253 mL | 0.1263 mL | 0.2525 mL | 0.6313 mL | |
| 100 mM | 0.0202 mL | 0.1010 mL | 0.2020 mL | 0.5050 mL |