HER2-IN-9
HER2-IN-9 is an orally active HER2 inhibitor, with an IC50 value of 0.03 μM. HER2-IN-9 inhibits HER-2 positive breast cancer cells proliferation and migration. HER2-IN-9 can be used in the research of breast cancers.
For research use only. We do not sell to patients.
- Formula: C19H14BrF3N2O
- Molecular Weight:423.23
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All EGFR Isoforms
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Biological Activity
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HER2 0.03 μM (IC50) |
HER2-IN-9 (24 h) shows anti-proliferation activities against cancer cells (A549, HEPG2, MCF7, SKBR3)[1].
HER2-IN-9 (0-60 nM, 24 h) inhibits the migration of SKBR3 cells[1].
HER2-IN-9 (0-60 nM, 24 h) increases E-cadherin levels and decreases N-cadherin levels in SKBR3 cells[1].
HER2-IN-9 (0-60 nM, 24 h) suppresses the expression of p-HER-2, further inhibits the activation of the EMT signal pathway to inhibit the migration of SKBR3 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Cancer cells (A549, HEPG2, MCF7, SKBR3), normal cells (Beas2b, LO2, MCF-0A)
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Concentration:0.05-30 μM approximately
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Incubation Time:24 h
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Result:Inhibited cancer cell proliferation with IC50s of 0.05-12.17 μM.
Inhibited noamal cell proliferation with IC50s of 15.4- 26.95 μM.
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Cell Line:SKBR3 cells
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Concentration:0, 20, 40, 60 nM
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Incubation Time:24 h
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Result:Inhibited HER-2 phosphorylation with no significant change in total HER-2 protein levels.
Down-regulated β-catenin, snail, and Vimentin level.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:SKBR3 orthotopic xenograft model[1]
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Dosage:30 mg/kg
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Administration:Oral administration, every two days.
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Result:Inhibited the growth of cancer cells in vivo without noticeable toxic effects.
Increased the level of cleaved-caspase 3 implicated in cell death pathways (immunohistochemistry assay in tumor).
Chemical Information
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Molecular Weight 423.23
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Formula C19H14BrF3N2O
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SMILES
FC(F)(C1=CC=C(C=C1)/C=C/C2=COC(CNC3=CC=C(C=C3)Br)=N2)F
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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)