EGFR kinase inhibitor 3
Based on 1 Customer Validation
EGFR kinase inhibitor 3 (compound 2) is a bivalent ATP-allosteric EGFR kinase inhibitor with IC50s of <10 nM, 1.5 nM, 0.059 nM, 0.064 nM for WT EGFR, EGFR-activating mutations L858R, L858R/T790M and L858R/T790M/C797S, respectively. EGFR kinase inhibitor 3 is a C-linked inhibitor.
For research use only. We do not sell to patients.
- Purity: 99.03%
- CAS No.: 2922402-03-5
- Formula: C31H25N7O3S
- Molecular Weight:575.64
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
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Biological Activity
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EGFR (WT) <10 nM (IC50) |
EGFR L858R 1.5 nM (IC50) |
EGFR L858R/T790M 0.059 nM (IC50) |
EGFR L858R/T790M/C797S 0.064 nM (IC50) |
Chemical Information
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CAS No. 2922402-03-5
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Appearance Solid
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Molecular Weight 575.64
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Formula C31H25N7O3S
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Color Light yellow to yellow
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SMILES
O=C(NC1=CC=CC(C2=C(NC(SC)=N2)C3=CC=NC(NC(C)=O)=C3)=C1)C4=C5NC(C6=C(NC5=CC=C4)C=CC=C6)=O
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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 (173.72 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.
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: ≥ 5 mg/mL (8.69 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
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 (280 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
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 | 1.7372 mL | 8.6860 mL | 17.3720 mL | 43.4299 mL |
| 5 mM | 0.3474 mL | 1.7372 mL | 3.4744 mL | 8.6860 mL | |
| 10 mM | 0.1737 mL | 0.8686 mL | 1.7372 mL | 4.3430 mL | |
| 15 mM | 0.1158 mL | 0.5791 mL | 1.1581 mL | 2.8953 mL | |
| 20 mM | 0.0869 mL | 0.4343 mL | 0.8686 mL | 2.1715 mL | |
| 25 mM | 0.0695 mL | 0.3474 mL | 0.6949 mL | 1.7372 mL | |
| 30 mM | 0.0579 mL | 0.2895 mL | 0.5791 mL | 1.4477 mL | |
| 40 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0857 mL | |
| 50 mM | 0.0347 mL | 0.1737 mL | 0.3474 mL | 0.8686 mL | |
| 60 mM | 0.0290 mL | 0.1448 mL | 0.2895 mL | 0.7238 mL | |
| 80 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5429 mL | |
| 100 mM | 0.0174 mL | 0.0869 mL | 0.1737 mL | 0.4343 mL |