1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis
  3. EGFR-IN-107

EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research.

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

EGFR-IN-107 Chemical Structure

EGFR-IN-107 Chemical Structure

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Description

EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. EGFR-IN-107 has anti-proliferative activity and can inhibit the proliferation of H1975 cells and induce their apoptosis. EGFR-IN-107 can be used in cancer research[1].

In Vitro

EGFR-IN-107 (compound 3r) has an IC50 value of 5 nM for EGFR kinase[1].
EGFR-IN-107 has an IC50 value of 1.9 μM against the Osimertinib (HY-15772 ) -resistant H1975 cell line (H1975OR)[1].
EGFR-IN-107 (1 μM, 24 h) induces apoptosis and inhibits cell migration in H1975 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 1 μM
Incubation Time: 24h
Result: Up-regulated the expression levels of Bax, cleaved caspase-3 and E-cadherin, and down-regulated the expression levels of matrix metalloproteinase-2 (MMP-2) and anti-apoptotic marker Bcl-2.
In Vivo

EGFR-IN-107 (compound 3r) (5, 10, 20 mg/kg; Oral gavage (p.o.); 21 days) has strong antitumor activity in H1975 xenografted mouse models and can significantly inhibit the proliferation of H1975 xenografted mouse models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: H1975 xenograft mouse model[1]
Dosage: 5, 10, 20 mg/kg
Administration: Oral gavage (p.o.); 21days
Result: At 20 mg/kg showed the same antitumor effect as Osimertinib (HY-15772) (20 mg/kg).
Leaded to the down-regulation of p-EGFR.
Did not cause significant weight loss or tissue damage.
Molecular Weight

593.69

Formula

C34H36FN7O2

SMILES

C=CC(NC1=C(C=C(C(NC2=NC(C3=C(N(C4=C3C=CC=C4)C)C5=CC=CC(F)=C5)=CC=N2)=C1)OC)N(CCN(C)C)C)=O

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Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
EGFR-IN-107
Cat. No.:
HY-163396
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