1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
    c-Met/HGFR
  3. EGFR-IN-8

EGFR-IN-8 

Cat. No.: HY-126320
Handling Instructions

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC.

For research use only. We do not sell to patients.

EGFR-IN-8 Chemical Structure

EGFR-IN-8 Chemical Structure

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Description

EGFR-IN-8 is a dual EGFR and c-Met inhibitor, compound 48. EGFR-IN-8 can be a promising candidate for further development to target EGFR TKI-resistant NSCLC[1].

IC50 & Target

EGFR; c-Met[1]

In Vitro

EGFR-IN-8 (0-20 μM; 24-72 hours) exhibits a time- and dose-dependent inhibitory effect on the viability of A549, PC9, H1975, CL68, and CL97 cells at different time intervals, with IC50 values ranging from 0.3 to 0.6 μM and 0.2-0.5 μM after 48 and 72 h of treatment respectively[1].
EGFR-IN-8 (0-0.6 μM; 48 hours) suppresses the expression of EGFR and c-Met in these five cell lines irrespective of their mutational status[1].

Cell Viability Assay[1]

Cell Line: A549, PC9, H1975, CL68, and CL97 cells
Concentration: 0-20 μM
Incubation Time: 24 hours, 48 hours, 72 hours
Result: Showed inhibitory effects on different cells.

Western Blot Analysis[1]

Cell Line: A549, PC9, H1975, CL68, and CL97 cells
Concentration: 0-0.6 μM
Incubation Time: 48 hours
Result: Decreased EGFR and c-Met expression.
In Vivo

EGFR-IN-8 (oral gavage; 50 and 150 mg/kg; once daily; 20 days) exhibits a dose-dependent suppression (29% and 60%, respectively) of H1975 xenograft tumor growth at 50 and 150 mg/kg[1].

Animal Model: Nude mice H1975 xenograft tumor model[1]
Dosage: 50 and 150 mg/kg
Administration: Oral gavage; 50 and 150 mg/kg; once daily; 20 days
Result: Inhibited H1975 xenograft tumor growth.
Molecular Weight

662.02

Formula

C₃₂H₂₃ClF₃N₇O₄

SMILES

O=C(NC1=CC(C(F)(F)F)=C(NC(C2CC2)=O)C=C1)NC3=CC=CC(C4=NC(C5=CC=C(NC(C6=CC=CN=C6)=O)C=C5Cl)=NO4)=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

EGFR-IN-8EGFRc-Met/HGFREpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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EGFR-IN-8
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HY-126320
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