EGFR-IN-186
EGFR-IN-186 is a potent inhibitor of EGFR with an IC50 of 0.065 µM. EGFR-IN-186 also exhibits inhibitory activity against EGFRL858R (IC50 = 0.528 µM) and EGFRT790M (IC50 = 0.465 µM). EGFR-IN-186 induces apoptosis by increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level. EGFR-IN-186 can be used for the research of non-small cell lung cancer (NSCLC).
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- Formule: C24H20N6O3S
- Masse moléculaire:472.52
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
[1]|
EGFR 0.065 μM (IC50) |
EGFRL858R 0.528 μM (IC50) |
EGFRT790M 0.465 μM (IC50) |
In Vitro
EGFR-IN-186 (compound 6) (48 h) exhibits potent cytotoxicity against A549, NCI-H460, and HOP-62 cancer cell lines (IC50 = 4.55, 26.09, and 10.72 μM, respectively), while showing significantly lower toxicity toward the normal human lung fibroblast cell line WI-38 (IC50 = 44.64 μM)[1].
EGFR-IN-186 (48 h) exhibits enhancement in its cytotoxicity against A-549 cells (IC50 = 2.38 μM after radiation), indicating that it shows a good radiosensitizing ability[1].
EGFR-IN-186 (4.55 μM; 48 h) induces apoptosis through increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level in A549 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A-549
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Concentration:4.55 μM
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Incubation Time:48 h
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Result:Caused a remarkable increase in early apoptosis from 0.79% (control) to 18.51%.
Showed an increase in the late cellular apoptosis from 0.18% (control) to 6.57%.
Induced early apoptosis in A-549 cells 1.65 folds better than Erlotinib (HY-50896).
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Cell Line:A-549
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Concentration:4.55 μM
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Incubation Time:48 h
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Result:Increased the level of pro-apoptotic protein Bax expression compared to control.
Down-regulated the level of the expression of anti-apoptotic protein Bcl-2 compared to control.
Increased the Bax/BCl-2 ratio.
Led to activation of caspase-3 and increased its expression level when compared to untreated control cells.
Chemical Information
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Masse moléculaire 472.52
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Formule C24H20N6O3S
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SMILES
O=C(NC=N1)C2=C1N(C=C2C3=CC=CC=C3)C4=CC=C(S(=O)(NC5=NC(C)=CC(C)=N5)=O)C=C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-186 Related Classifications
HY-179522 Related Classifications
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