EGFR-IN-60
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.
- CAS No.: 2699877-43-3
- Formula: C28H28Cl2N6O
- Molecular Weight:535.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All EGFR Isoforms
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Biological Activity
|
EGFR 0.083 μM (IC50) |
EGFRL858R 0.053 μM (IC50) |
EGFRT790M 0.026 μM (IC50) |
JAK3 0.069 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Hepatocellular (HepG2), Colorectal (HCT-116), Breast (MCF-7) cancer cells
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Concentration:3.25-88.46 μM
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Incubation Time:48 hours
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Result:Inhibited HepG2 cells, HCT-116 cells, MCF-7 cells with IC50values of 4.46 μM, 5.27 μM and 3.25 μM respectively.
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Cell Line:Overexpress EGFRWT human epidermoid carcinoma cells (A431), Mutant EGFRT790M cells NSCLC (H1975), Lung fibroblast cells (WI38), Amnion epithelial cells (WISH)
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Concentration:0.49-86.4 μM
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Incubation Time:48 hours
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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.
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Cell Line:HepG2, HCT-116, MCF-7
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Concentration:0 μM, 3.25 μM, 4.46 μM, 5.27 μM
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Incubation Time:24 hours
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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.
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Cell Line:HepG2, HCT-116, MCF-7
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Concentration:3.25 μM, 4.46 μM, 5.27 μM
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Incubation Time:24 hours
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Result:Induced more apoptosis in MCF-7 cells comparing with HepG2 and HCT-116 cells.
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Cell Line:HepG2, HCT-116, MCF-7
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Concentration:0 µM, 10 µM
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Incubation Time:24 hours
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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.
Chemical Information
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CAS No. 2699877-43-3
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Molecular Weight 535.47
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Formula C28H28Cl2N6O
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-60 Related Classifications
HY-147826 Related Classifications
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