EGFR kinase inhibitor 1
EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity.
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- CAS No.: 2413958-04-8
- Formula: C30H31N7O2
- Molecular Weight:521.61
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
|
EGFR (WT) 37 nM (IC50) |
EGFRL858R/T790M 1.7 nM (IC50) |
EGFRL858R/T790M/C797S >300 nM (IC50) |
EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively[1].
EGFR kinase inhibitor 1 (0.05, 0.5, 5 µM; 48 h) induces apoptosis in a dose-dependent manner[1].
EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase[1].
EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, H1975 cells
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Concentration:
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Incubation Time:72 h
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Result:Showed antiproliferation activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively.
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Cell Line:H1975 cells
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Concentration:0.05, 0.5, 5 µM
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Incubation Time:48 h
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Result:Induced apoptosis in a dose-dependent manner.
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Cell Line:H1975 cells
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Concentration:4, 20, 100 nM
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Incubation Time:48 h
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Result:Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM.
Chemical Information
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CAS No. 2413958-04-8
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Molecular Weight 521.61
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Formula C30H31N7O2
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SMILES
C=CC(NC1=C(C=C(C(NC2=NC(C3=CN(C4=C3C=CC=C4)C)=CC=N2)=C1)OC)N5C=CC=C5CN(C)C)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR kinase inhibitor 1 Related Classifications
HY-143246 Related Classifications
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