EGFR-IN-185
EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of NSCLC.
For research use only. We do not sell to patients.
- Formula: C30H28FN3O2
- Molecular Weight:481.56
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
EGFR-IN-185 (compound 33) (48 h) exhibits antiproliferation activity against NSCLC cells, with IC50s of 3.1 (HCC827), 5.2 (H1975), 2.7 (H1975TM), and 10.2 μM (A549)[1].
EGFR-IN-185 (1-9 μM; 48 h) arrests the cell cycle progression of H1975TM cells at the G0/G1 phase in a concentration-dependent manner[1].
EGFR-IN-185 (0-10 μM; 0-24 h) inhibits H1975TM cell migration in a concentration-dependent manner[1].
EGFR-IN-185 shows negligible inhibitory activity against EGFRWT, EGFR19del, EGFRL858R/T790M and EGFRL858R/T790M/C797S, with IC50 values of approximately 100, 20, 4, and 44 μM, respectively, suggesting that it does not function as an allosteric EGFR tyrosine kinase inhibitor[1].
EGFR-IN-185 (2-10 μM, 20 h) exhibits strong antiproliferative effects on H1975TM cells and suppresses the EGFR signaling pathway, as evidenced by the reduction of EGFR and AKT phosphorylation[1].
EGFR-IN-185 (0-9 μM, 10 days) inhibits colony formation of H1975™ cells in a concentration-dependent manner[1].
EGFR-IN-185 (2-8 μM, 32 h) inhibits H1975TM cell growth through inducing cell apoptosis in a concentration-dependent
manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:H1975™
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Concentration:1, 3, 6, and 9 μM
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Incubation Time:48 h
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Result:Increased the percentage of H1975™ cells in the G0/G1 phase and decreased the S and G2/M phases. Increased the G0/G1 phase at 9 μM from 30.8% (control) to 59.7%, while it decreased S and G2/M phases from 50.3% and 18.9% to 31.1% and 9.3%, respectively.
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Cell Line:H1975™
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Concentration:0, 2, 4, 6, 10 μM
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Incubation Time:0, 12, and 24 h
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Result:Inhibited H1975™ cell migration in a concentration-dependent manner. Exhibited only 12% and 22% wound closure at 10 μM after 12 and 24 h.
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Cell Line:H1975™
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Concentration:2, 6, and 10 μM
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Incubation Time:20 h
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Result:Suppressed the phosphorylation of EGFR and its downstream proteins Akt in H1975™ cells in a concentration dependent manner. Significantly decreased the expression of p-EGFR by 59% and p-Akt by 57% at 10 μM. Did not target the downstream PI3Kα and AKT1 kinases of the EGFR pathway.
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Cell Line:H1975™
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Concentration:0, 1, 2, 4, 6, and 9 μM
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Incubation Time:10 days
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Result:Inhibited colony formation of H1975™ cells in a concentration dependent manner. Exhibited a good inhibitory effect on the colony formation of H1975™ cells at concentrations above its IC₅₀ value (2.66 µM). Showed almost no colony formation at 9 μM.
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Cell Line:H1975™
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Concentration:2, 6, and 8 μM
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Incubation Time:32
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Result:Induced apoptosis in H1975™ cells in a concentration-dependent manner, increasing both early and late apoptotic populations. Increased the early and late apoptosis states at 8 μM from 1.11% and 2.51% (control) to 18.26% and 55.05%, respectively.
Chemical Information
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Molecular Weight 481.56
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Formula C30H28FN3O2
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SMILES
O=C1C2=CC(OCC3=CC=C(C4=CC=CC=C4)C=C3)=CC=C2NC5=C(C=C(F)C=C5)N1CCN(C)C
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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)