EGFR-IN-197
EGFR-IN-197 is an EGFR inhibitor with IC50 values of 19.5 nM and 12.0 nM against EGFRL858R/T790M and EGFRL858R/T790M/C797S, respectively. EGFR-IN-197 arrests the cell cycle of NCI-H1975 cells at the G2/M phase, while inhibiting their proliferation, colony formation and migration; it also inhibits mitochondrial translocation and upregulates mitochondrial H2S levels. EGFR-IN-197 disrupts anti-apoptotic signaling pathways by regulating apoptosis-related proteins; it induces DNA damage and activates pro-apoptotic pathways to trigger apoptosis. EGFR-IN-197 can be used in studies related to non-small cell lung cancer (NSCLC).
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- No. CAS: 3060883-16-8
- Fòrmula: C23H26BrN7O2
- Peso molecular:512.40
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
EGFRL858R/T790M 19.5 nM (IC50) |
EGFRL858R/T790M/C797S 12.0 nM (IC50) |
ERK |
PARP |
Caspase 3 |
Bcl-xL |
In Vitro
EGFR-IN-197 (compound 6e) (72 h) potently inhibits proliferation of NCI-H1975, HCC827, and A431 cells with IC50 values of 0.0473 μM, 0.0185 μM, and 0.0226 μM, respectively[1].
EGFR-IN-197 potently inhibits EGFRL858R/T790M and EGFRL858R/T790M/C797S mutant kinases with IC50 values of 19.5 nM and 12.0 nM, respectively[1].
EGFR-IN-197 (0.05-0.5 μM; 14 d) concentration-dependently inhibits colony formation of NCI-H1975 cells[1].
EGFR-IN-197 (0.05-0.5 μM; 12 h, 24 h) concentration-dependently inhibits migration of NCI-H1975 cells[1].
EGFR-IN-197 (0.05-0.5 μM, 24 h) disrupts mitochondrial translocation of EGFR in NCI-H1975 cells[1].
EGFR-IN-197 (0.05-0.5 μM, 24 h) concentration-dependently upregulates mitochondrial H2S levels in NCI-H1975 cells[1].
EGFR-IN-197 (0.005-0.5 μM; 24 h) concentration-dependently inhibits phosphorylation of EGFR and ERK1/2 in NCI-H1975 cells, and significantly inhibits AKT phosphorylation at 0.5 μM[1].
EGFR-IN-197 (0.005-0.5 μM; 24 h) concentration-dependently modulates apoptosis-related proteins in NCI-H1975 cells, increasing Cleaved PARP and Cleaved caspase-3 and decreasing Bcl-xL[1].
EGFR-IN-197 (0.1-1 μM; 24 h) concentration-dependently induces apoptosis in NCI-H1975 cells, with strong induction of late apoptosis at 0.5 μM and above[1].
EGFR-IN-197 (0.05-0.5 μM; 24 h) concentration-dependently arrests NCI-H1975 cells at the G2/M phase, with 62.29% of cells in G2/M phase at 0.5 μM[1].
EGFR-IN-197 (0.05-0.5 μM; 72 h) induces DNA damage in NCI-H1975 cells in a concentration-dependent manner, with significant damage observed at 0.1 μM and above[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H1975 cells
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Concentration:0.05 μM, 0.1 μM, 0.5 μM
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Incubation Time:14 d
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Result:Concentration-dependently suppressed colony formation of NCI-H1975 cells.
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Cell Line:NCI-H1975 cells
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Concentration:0.05 μM, 0.1 μM, 0.5 μM
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Incubation Time:72 h
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Result:Significantly inhibited migration of NCI-H1975 cells, with effects detectable at 0.05 μM.
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Cell Line:NCI-H1975 cells
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Concentration:0.05 μM, 0.1 μM, 0.5 μM
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Incubation Time:12 h, 24 h
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Result:EGFR-IN-197 concentration-dependently inhibits migration of NCI-H1975 cells.
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Cell Line:NCI-H1975 cells
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Concentration:0.005 μM, 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM
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Incubation Time:24 h
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Result:Concentration-dependently suppressed phosphorylation of EGFR (p-EGFR) and ERK1/2 (p-ERK1/2) in NCI-H1975 cells.
Significantly inhibited phosphorylation of AKT (p-AKT) at 0.5 μM.
Concentration-dependently increased expression of Cleaved PARP and Cleaved caspase-3, and decreased expression of Bcl-xL in NCI-H1975 cells.
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Cell Line:NCI-H1975 cells
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Concentration:0.1 μM, 0.5 μM, 1 μM
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Incubation Time:24 h
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Result:Concentration-dependently induced apoptosis in NCI-H1975 cells.
Increased the proportion of late apoptotic cells sharply at 0.5 μM.
Induced late apoptosis in 30.5% of cells and early apoptosis in 0.73% of cells at 1 μM.
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Cell Line:NCI-H1975 cells
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Concentration:0.05 μM, 0.1 μM, 0.5 μM
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Incubation Time:24 h
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Result:Concentration-dependently arrested NCI-H1975 cells at the G2/M phase.
Resulted in 36.42% of cells in G0/G1 phase and 32.14% in G2/M phase at 0.05 μM.
Resulted in 20.85% of cells in G0/G1 phase and 54.52% in G2/M phase at 0.1 μM.
Resulted in 12.40% of cells in G0/G1 phase and 62.29% in G2/M phase at 0.5 μM.
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Cell Line:NCI-H1975 cells
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Concentration:0.05 μM, 0.1 μM, 0.5 μM
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Incubation Time:24 h
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Result:EGFR-IN-197 disrupts mitochondrial translocation of EGFR in NCI-H1975 cells.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Cell migration
- Apoptosis Solutions
- Protocol for Cell Cycle
- Soft Agar Colony Formation Assay
- Colony Formation (Clonogenic) Assay
- Genotoxicity/Mutagenicity Study
- Cell Viability Determination by MTT Colorimetric Assay
Chemical Information
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No. CAS 3060883-16-8
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Peso molecular 512.40
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Fòrmula C23H26BrN7O2
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SMILES
CN(CC1)CCN1C(C=C2)=CC=C2NC3=NC=C(Br)C(NC4=CC=CC=C4C(NOC)=O)=N3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- EGFR-IN-197
- 3060883-16-8
- EGFR
- ERK
- PARP
- Caspase
- Bcl-2 Family
- Apoptosis
- EGFR inhibitor
- G2/M phase cell cycle arrest
- induce DNA damage and apoptosis
- regulate apoptosis-related proteins
- inhibit colony formation and cell migration
- inhibit EGFR mitochondrial translocation
- upregulate mitochondrial H?S levels
- non-small cell lung cancer (NSCLC)
- NCI-H1975 cells
- HCC827 cells
- A431 cells
- Inhibitor
- inhibitor
- inhibit