EGFR-IN-89
Based on 1 Customer Validation
EGFR-IN-89 (compound 13k) is a potent, fourth-generation EGFR mutation inhibitor with an IC50 of 10.1 nM against Del19/T790M/C797S mutations. EGFR-IN-89 shows higher selectivity over wild type.
For research use only. We do not sell to patients.
- Purity: 98.75%
- CAS No.: 2413029-40-8
- Formula: C26H31FN8O2S
- Molecular Weight:538.64
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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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EGFR19del/TM/CS 10.1 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
333.8 nM
Compound: 13k
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Antiproliferative activity against human A-431 cells harboring wild type EGFR incubated for 72 hrs by SRB assay
Antiproliferative activity against human A-431 cells harboring wild type EGFR incubated for 72 hrs by SRB assay
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[PMID: 37783102] |
| HCC827 | IC50 |
121.1 nM
Compound: 13k
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Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant incubated for 72 hrs by SRB assay
Antiproliferative activity against human HCC827 cells harboring EGFR Del19 mutant incubated for 72 hrs by SRB assay
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[PMID: 37783102] |
| NCI-H1975 | IC50 |
178.2 nM
Compound: 13k
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by SRB assay
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[PMID: 37783102] |
| NCI-H1975 | IC50 |
201.6 nM
Compound: 13k
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Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by SRB assay
|
[PMID: 37783102] |
| PC-9 | IC50 |
154.8 nM
Compound: 13k
|
Antiproliferative activity against human PC-9 cells harboring EGFR Del19/T790M/C797S mutant incubated for 72 hrs by SRB assay
Antiproliferative activity against human PC-9 cells harboring EGFR Del19/T790M/C797S mutant incubated for 72 hrs by SRB assay
|
[PMID: 37783102] |
Chemical Information
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CAS No. 2413029-40-8
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Appearance Solid
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Molecular Weight 538.64
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Formula C26H31FN8O2S
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Color White to off-white
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SMILES
FC1=CC(NC2=NC(NC3=C(N(C)S(=O)(C)=O)C=CC=C3)=C4C(NC=C4)=N2)=CC=C1N5CCN(CC)CC5
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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 (185.65 mM; ultrasonic and warming and heat to 60°C; 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 (9.28 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 (274 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 | 1.8565 mL | 9.2826 mL | 18.5653 mL | 46.4132 mL |
| 5 mM | 0.3713 mL | 1.8565 mL | 3.7131 mL | 9.2826 mL | |
| 10 mM | 0.1857 mL | 0.9283 mL | 1.8565 mL | 4.6413 mL | |
| 15 mM | 0.1238 mL | 0.6188 mL | 1.2377 mL | 3.0942 mL | |
| 20 mM | 0.0928 mL | 0.4641 mL | 0.9283 mL | 2.3207 mL | |
| 25 mM | 0.0743 mL | 0.3713 mL | 0.7426 mL | 1.8565 mL | |
| 30 mM | 0.0619 mL | 0.3094 mL | 0.6188 mL | 1.5471 mL | |
| 40 mM | 0.0464 mL | 0.2321 mL | 0.4641 mL | 1.1603 mL | |
| 50 mM | 0.0371 mL | 0.1857 mL | 0.3713 mL | 0.9283 mL | |
| 60 mM | 0.0309 mL | 0.1547 mL | 0.3094 mL | 0.7736 mL | |
| 80 mM | 0.0232 mL | 0.1160 mL | 0.2321 mL | 0.5802 mL | |
| 100 mM | 0.0186 mL | 0.0928 mL | 0.1857 mL | 0.4641 mL |