1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. EGFR-IN-11

EGFR-IN-11 

Cat. No.: HY-130616
Handling Instructions

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1.

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EGFR-IN-11 Chemical Structure

EGFR-IN-11 Chemical Structure

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Description

EGFR-IN-11 is a fourth-generation EGFR-tyrosine kinase inhibitor (EGFR-TKI) with an IC50 of 18 nM for triple mutant EGFRL858R/T790M/C797S. EGFR-IN-11 significantly suppresses the EGFR phosphorylation, induce the apoptosis, and arrest cell cycle at G0/G1[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

18 nM (IC50)

In Vitro

EGFR-IN-11 (Compound D9; 0.0001-10 µM; 72 hours) shows significantly potent anti-proliferation against HCC827 and H1975 cell lines with IC50s of 0.88 nM and 0.20 µM, respectively[1].
EGFR-IN-11 (0.01-1.00 µM for HCC827 cells; 0.1-10.00 µM for H1975 and A549 cells; 8 hours) suppresses EGFR phosphorylation in a concentration-dependent manner in the HCC827, H1975 and A549 cell line[1].
EGFR-IN-11 (1 µM; 24 h) potently induces the apoptosis of HCC827 cells.[1]
EGFR-IN-11 (1 µM; 24 h) induces cell cycle arrests in HCC827 cell[1].

Cell Proliferation Assay[1]

Cell Line: Human lung cancer cell lines HCC827 (EGFRDel E746-A750), H1975 (EGFRL858R/T790M) and A549 (EGFRWT); epidermoid carcinoma cell line A431 (EGFRWT)
Concentration: 0.0001, 0.0003, 0.001, 0.003, 0.01, 0.1, 1, 10 µM
Incubation Time: 72 hours
Result: Inhibited HCC827 H1975 A549 cells proliferation with IC50s of 0.88±0.09 nM, 0.20±0.01 μM, 2.91±0.61 μM, and >10 μM, respectively.

Western Blot Analysis[1]

Cell Line: HCC827, H1975 and A549 cells
Concentration: 1.00, 0.10 and 0.01 µM for HCC827 cells; 10.00, 1.00 and 0.10 µM for H1975 and A549 cells
Incubation Time: 8 hours
Result: Suppressed EGFR phosphorylation in a concentration-dependent manner. EGFR phosphorylation in the HCC827 cell line was more remarkably suppressed than in the H1975 and A549 cell lines.

Apoptosis Analysis[1]

Cell Line: HCC827 cells
Concentration: 1 µM
Incubation Time: 24 hours
Result: The percentages of apoptotic cells is 56.91%.

Cell Cycle Analysis[1]

Cell Line: HCC827 cells
Concentration: 1 µM
Incubation Time: 24 hours
Result: The number of HCC827 cells in G0/G1 phase was increased significantly.
Molecular Weight

573.71

Formula

C₂₉H₃₅N₉O₂S

SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C=N3)N=C(NC5=CC=CC=C5)N4[[email protected]]6CN(CC6)S(C7CC7)(=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

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Keywords:

EGFR-IN-11EGFREpidermal growth factor receptorErbB-1HER1EGFR-TKItriplemutantL858RT790MC797SNSCLClungcancerInhibitorinhibitorinhibit

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EGFR-IN-11
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