1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. EGFR
    Apoptosis
  3. EGFR-IN-60

EGFR-IN-60 

Cat. No.: HY-147826
Handling Instructions

EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio.

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

EGFR-IN-60 Chemical Structure

EGFR-IN-60 Chemical Structure

CAS No. : 2699877-43-3

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Description

EGFR-IN-60 (Compound 7d) shows obvious inhibition of EGFRWT, EGFRT790M, EGFRL858R and JAK3 with IC50s of 83, 26, 53, and 69 nM, respectively. EGFR-IN-60 potently inhibits the growth of H1975 cells harboring EGFRT790M mutation (IC50=1.32 µM) over A431 cells overexpressing EGFRWT (IC50=4.96 µM). EGFR-IN-60 exhibits good oral absorption, potent and safe antitumor activity. EGFR-IN-60 induces cell death through apoptosis supported by increased Bax/Bcl-2 ratio[1].

IC50 & Target

EGFR

0.083 μM (IC50)

EGFRL858R

0.053 μM (IC50)

EGFRT790M

0.026 μM (IC50)

JAK3

0.069 μM (IC50)

In Vitro

EGFR-IN-60 (compound 7d) (3.25-88.46 μM, 48 hours) shows well antitumor activity against hepatocellular (HepG2), colorectal (HCT-116) and breast (MCF-7) cancer cells[1].
EGFR-IN-60 (compound 7d) (0.49-86.4 μM, 48 hours) shows cytotoxic activity against cancer cells[1].
EGFR-IN-60 (compound 7d) (0-5.27 μM, 24 hours) induces an increase in G2/M phase cells and induces apoptosis in HepG2, HCT-116, and MCF-7 cell lines[1].
EGFR-IN-60 (compound 7d) (0 µM, 10 µM, 24 hours) can induce apoptosis through up-regulation of Bax and down-regulation of Bcl-2[1].

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

Cell Proliferation Assay[1]

Cell Line: Hepatocellular (HepG2), Colorectal (HCT-116), Breast (MCF-7) cancer cells
Concentration: 3.25-88.46 μM
Incubation Time: 48 hours
Result: Inhibited HepG2 cells, HCT-116 cells, MCF-7 cells with IC50values of 4.46 μM, 5.27 μM and 3.25 μM respectively.

Cell Cytotoxicity Assay[1]

Cell Line: Overexpress EGFRWT human epidermoid carcinoma cells (A431), Mutant EGFRT790M cells NSCLC (H1975), Lung fibroblast cells (WI38), Amnion epithelial cells (WISH)
Concentration: 0.49-86.4 μM
Incubation Time: 48 hours
Result: Showed cytotoxic activity against A431, H1975, WI38, WISH with IC50 value of 4.96 μM, 1.32 μM, 64.27 μM, 46.38 μM respectively.

Cell Cycle Analysis[1]

Cell Line: HepG2, HCT-116, MCF-7
Concentration: 0 μM, 3.25 μM, 4.46 μM, 5.27 μM
Incubation Time: 24 hours
Result: Resulted in an increase in the percentage of G2/M phase cells from 14.09% to 25.66% , from 15.87% to 38.51%, from 10.95% to 41.60% in HepG2, HCT-116, MCF-7 cell lines respectively.

Apoptosis Analysis[1]

Cell Line: HepG2, HCT-116, MCF-7
Concentration: 3.25 μM, 4.46 μM, 5.27 μM
Incubation Time: 24 hours
Result: Induced more apoptosis in MCF-7 cells comparing with HepG2 and HCT-116 cells.

Western Blot Analysis[1]

Cell Line: HepG2, HCT-116, MCF-7
Concentration: 0 µM, 10 µM
Incubation Time: 24 hours
Result: Showed the levels of pro-apoptotic protein Bax upgrading by 5.71, 8.15 and 16.51 fold and the levels of anti-apoptotic protein Bcl-2 down-regulating by 0.72, 0.53 and 0.31 fold in HepG2, HCT-116, MCF-7, respectively.
Molecular Weight

535.47

Formula

C28H28Cl2N6O

CAS No.
SMILES

O=C1C2=C(NC(N=CN(/N=C/C3=CC=C(N(C)C)C=C3)C4=N)=C4C2C5=CC=CC(Cl)=C5Cl)CC(C)(C)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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EGFR-IN-60
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