EGFR T790M/L858R-IN-8
Based on 1 Customer Validation
EGFR T790M/L858R-IN-8 (Compound 9) is a selective EGFRT790M/L858R mutant kinase inhibitor with a IC50 of 56.8 μM, and it shows no inhibitory activity against wild-type EGFR. EGFR T790M/L858R-IN-8 can be used for the research of non-small cell lung cancer.
For research use only. We do not sell to patients.
- Purity: 99.20%
- CAS No.: 333419-97-9
- Formula: C16H11BrN2O3
- Molecular Weight:359.17
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EGFR (L858R/T790M) 56.8 μM (IC50) |
Cellular Effect
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
>100 μM
Compound: 9
|
Antiproliferative activity against human A431 cells over-expressing EGFR gene after 72 hrs by SRB assay
Antiproliferative activity against human A431 cells over-expressing EGFR gene after 72 hrs by SRB assay
|
[PMID: 22227214] |
| A549 | IC50 |
>100 μM
Compound: 9
|
Antiproliferative activity against human A549 cells over-expressing EGFR gene after 72 hrs by SRB assay
Antiproliferative activity against human A549 cells over-expressing EGFR gene after 72 hrs by SRB assay
|
[PMID: 22227214] |
| NCI-H1975 | IC50 |
>100 μM
Compound: 9
|
Antiproliferative activity against human NCI-H1975 cells over-expressing EGFR mutant gene after 72 hrs by SRB assay
Antiproliferative activity against human NCI-H1975 cells over-expressing EGFR mutant gene after 72 hrs by SRB assay
|
[PMID: 22227214] |
In Vitro
EGFR T790M/L858R-IN-8 selectively inhibits EGFRT790M/L858R mutant tyrosine kinase with an IC50 of 56.8 μM, while exhibiting no inhibition of wild-type EGFR at concentrations up to 100.0 μM[1].
EGFR T790M/L858R-IN-8 does not inhibit the proliferation of A549, A431, or NCI-H1975 cells at concentrations up to 100.0 μM[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. 333419-97-9
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Appearance Solid
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Molecular Weight 359.17
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Formula C16H11BrN2O3
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Color White to off-white
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SMILES
O=C(C1=C(O)C2=C(C=CC=C2)NC1=O)NC3=CC(Br)=CC=C3
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
In Vitro:
DMSO : 2 mg/mL (5.57 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)
Purity & Documentation
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Data Sheet (272 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 | 2.7842 mL | 13.9210 mL | 27.8420 mL | 69.6049 mL |
| 5 mM | 0.5568 mL | 2.7842 mL | 5.5684 mL | 13.9210 mL |