2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. 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.

HER2-IN-9 Chemical Structure

HER2-IN-9 Chemical Structure

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HER2-IN-9 Related Antibodies

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

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Description

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[1].

IC50 & Target[1]

HER2

0.03 μM (IC50)

In Vitro

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.

HER2-IN-9 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Cancer cells (A549, HEPG2, MCF7, SKBR3), normal cells (Beas2b, LO2, MCF-0A)
Concentration: 0.05-30 μM approximately
Incubation Time: 24 h
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.

Western Blot Analysis[1]

Cell Line: SKBR3 cells
Concentration: 0, 20, 40, 60 nM
Incubation Time: 24 h
Result: Inhibited HER-2 phosphorylation with no significant change in total HER-2 protein levels.
Down-regulated β-catenin, snail, and Vimentin level.
In Vivo

HER2-IN-9 (oral administration, 30 mg/kg, every two days) inhibits tumor growth SKBR3 orthotopic xenograft model[1].

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

Animal Model: SKBR3 orthotopic xenograft model[1]
Dosage: 30 mg/kg
Administration: Oral administration, every two days.
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).
Molecular Weight

423.23

Formula

C19H14BrF3N2O
SMILES

FC(F)(C1=CC=C(C=C1)/C=C/C2=COC(CNC3=CC=C(C=C3)Br)=N2)F
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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HER2-IN-9 Related Classifications

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Help & FAQs
  • 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.

Keywords:

HER2-IN-9EGFREpidermal growth factor receptorErbB-1HER1Cancerbreast cancermigrationEMTSKBR3MCF7p-HER-2Inhibitorinhibitorinhibit

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