1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  2. EGFR Apoptosis
  3. EGFR-IN-165

EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFRL858R/T790M and EGFRWT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

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EGFR-IN-165 Chemical Structure

EGFR-IN-165 Chemical Structure

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Description

EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFRL858R/T790M and EGFRWT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma[1].

In Vitro

EGFR-IN-165 (Compound 4b) (0-5 μM, 48 h) effectively inhibits EGFR phosphorylation in a concentration-dependent manner in A431 cells and NCI-H1975 cells[1].
EGFR-IN-165 (1.25-10 μM, 24 h) effectively inhibits the migration of A431 cells at a concentration of 10 μM[1].
EGFR-IN-165 (2.5-20 μM, 48 h) reaches 12.91% apoptosis rate in NCI-H1975 cells at a concentration of 20 μM[1].
EGFR-IN-165 (2.5-20 μM, 24-48 h) induces cell cycle arrest in the G1 phase of NCI-H1975 cells[1].
EGFR-IN-165 has superior stability with a half-life of 38.5 h in human plasma and a low clearance rate in liver microsomes with an intrinsic clearance rate of 24.3 mL/min/kg[1].

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

Western Blot Analysis[1]

Cell Line: A431 and NCI-H1975 cells
Concentration: 0, 1.25, 2.5, 5 μM
Incubation Time: 48 h
Result: Demonstrated significant and concentration-dependent inhibition of EGFR phosphorylation in A431 cells.
Exhibited effective and concentration-dependent inhibition of EGFR phosphorylation.

Cell Migration Assay [1]

Cell Line: A431 cells
Concentration: 1.25, 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Effectively inhibited the migration at a concentration of 10 μM.

Apoptosis Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 2.5, 5, 10 and 20 μM
Incubation Time: 48 h
Result: Reached 12.91% apoptosis rate in NCI-H1975 cells at a concentration of 20 μM.

Cell Cycle Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 2.5, 5, 10 and 20 μM
Incubation Time: 24-48 h
Result: The proportion of the G1 phase increased to 73.09 %, while the S phase decreased to 17.29 % and the G2 phase to 9.48 %.
Molecular Weight

483.48

Formula

C26H21N5O5

SMILES

COC1=C(C=C2C(N=CN=C2NC3=CC=C(C(C)=C3)C(OC4=NN=C(O4)C5=CC=CC=C5)=O)=C1)OC

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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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  • 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-165
Cat. No.:
HY-175011
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