EGFR-IN-451
EGFR-IN-451 is an EGFR inhibitor with an IC50 value of 0.02 nM. EGFR-IN-451 also inhibits mutant EGFRL858R, EGFRT790M, and EGFRL858R/T790M with IC50 values of 0.26-34 nM. EGFR-IN-451 inhibits AKT and ERK activation and inhibits proliferation of EGFR-mutant cancer cells. EGFR-IN-451 can be used for the research of EGFR-driven cancer.
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- CAS. Nr.: 220576-72-7
- Formel: C19H15N5O
- Molecular Weight:329.36
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
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Biologische Aktivität
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EGFR 0.02 nM (IC50) |
EGFRL858R 0.26 nM (IC50) |
EGFRT790M 25 nM (IC50) |
EGFRL858R/T790M 34 nM (IC50) |
EGFR-IN-451 (Compound R14) (0.1-10000 nM) potently inhibits wild-type EGFR (IC50 = 0.02 nM), EGFRL858R (IC50 = 0.26 nM), EGFRT790M (IC50 = 25 nM), and EGFRL858R/T790M (IC50 = 34 nM) in a cell-free caliper mobility shift assay[1].
EGFR-IN-451 inhibits the viability of HCC827 cells (IC50 = 2.47 μM) and H1975 cells (IC50 = 18.07 μM) in an MTT assay[1].
EGFR-IN-451 (0.01-10 μM; 1-12 h) inhibits phosphorylated EGFR in HCC827 cells at 0.01 μM and in H1975 cells at 0.1, 1, and 10 μM, with sustained reduction of phosphorylated EGFR in HCC827 cells over 12 h, and inhibits P-AKT, P-ERK expression[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCC827 cells, H1975 cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:1, 4, 8, 12 h (time-course in HCC827 cells)
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Result:Inhibited phosphorylated EGFR in HCC827 cells at 0.01, 0.1 μM.
Reduced phosphorylated EGFR levels in HCC827 cells at 1, 4, 8, and 12 h post-treatment.
Inhibited phosphorylated EGFR in H1975 cells at 0.1, 1, and 10 μM.
Reduced P-AKT, P-ERK expression.
Chemical Information
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CAS. Nr. 220576-72-7
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Molecular Weight 329.36
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Formel C19H15N5O
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SMILES
C=CC(NC1=CC2=C(N=CN=C2C=C1)NC3=CC4=C(C=C3)NC=C4)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
EGFR-IN-451 Related Classifications
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