1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis
  3. EGFR-IN-207

EGFR-IN-207 (Compound 5h) is an epidermal growth factor receptor (EGFR) kinase inhibitor with an IC50 of 0.21 μM. EGFR-IN-207 induces cell cycle arrest at the Sub-G1 phase and promotes Apoptosis. EGFR-IN-207 exhibits anticancer activity against lung cancer. EGFR-IN-207 shows extremely low toxicity in non-cancerous cell lines. EGFR-IN-207 can be used in lung cancer-related research.

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EGFR-IN-207

EGFR-IN-207 Chemical Structure

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Description

EGFR-IN-207 (Compound 5h) is an epidermal growth factor receptor (EGFR) kinase inhibitor with an IC50 of 0.21 μM. EGFR-IN-207 induces cell cycle arrest at the Sub-G1 phase and promotes Apoptosis. EGFR-IN-207 exhibits anticancer activity against lung cancer. EGFR-IN-207 shows extremely low toxicity in non-cancerous cell lines. EGFR-IN-207 can be used in lung cancer-related research[1].

In Vitro

EGFR-IN-207 potently inhibits the kinase activity of wild-type EGFR with an IC50 of 0.21 ± 0.06 μM, and exhibits better efficacy than Erlotinib (HY-50896)[1].
EGFR-IN-207 (0.1-100 μM; 72 h) results in cell viabilities of 82% and 83% in HBEC30KT and HEK293 cells, respectively, at the concentration of 10 μM[1].
EGFR-IN-207 (0.5-10 μM; 72 h) potently and concentration-dependently inhibits the proliferation of H1975 and A549 human lung cancer cells[1].
EGFR-IN-207 (5 μM; 24 h) induces robust Sub-G1 cell cycle arrest and apoptosis in human lung cancer cell lines H1975 and A549[1].

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

Cell Proliferation Assay[1]

Cell Line: H1975 EGFR L858R/T790M mutant cells, A549 EGFR wild-type cells
Concentration: 0.5-10 μM
Incubation Time: 72 h
Result: Reduced viable cell percentage to 86% at 1 μM, 34% at 5 μM, and 27% at 10 μM in H1975 cells, surpassing erlotinib's effect (37% viability at 10 μM).
Reduced viable cell percentage to 91% at 1 μM and 36% at 10 μM in A549 cells, with activity comparable to erlotinib.

Apoptosis Analysis[1]

Cell Line: H1975, A549 human lung cancer cells
Concentration: 5 μM
Incubation Time: 24 h
Result: Increased the apoptotic cell population to 18.7 ± 1.9% (from 1.9 ± 0.4% in control) in H1975 cells, exceeding erlotinib's effect (13.7 ± 3.2%).
Increased the apoptotic cell population to 15.8 ± 2.1% (from 2.1 ± 0.2% in control) in A549 cells, with activity comparable to erlotinib.
Molecular Weight

427.26

Formula

C20H13Cl2FN6

SMILES

CC1=NN(C2=CC=C(F)C=C2)C3=C1C4=C(N=NN4C5=CC(Cl)=CC(Cl)=C5)C(C)=N3

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
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  • 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-207
Cat. No.:
HY-182073
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