1. JAK/STAT Signaling
    Protein Tyrosine Kinase/RTK
    Apoptosis
  2. EGFR
    Apoptosis
  3. EGFR/HER2-IN-6

EGFR/HER2-IN-6 

Cat. No.: HY-151156
Handling Instructions

EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer.

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

EGFR/HER2-IN-6 Chemical Structure

EGFR/HER2-IN-6 Chemical Structure

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Description

EGFR/HER2-IN-6 (compound 43) is an EGFR/HER2 and DHFR inhibitor. EGFR/HER2-IN-6 inhibits EGFR kinase, HER2 kinase and DHFR with IC50s of 0.122, 0.078 and 0.585 μM, respectively. EGFR/HER2-IN-6 shows anticancer activity against several cancer cell lines with high safety profile and selectivity indices. EGFR/HER2-IN-8 can be used for the research of cancer[1].

IC50 & Target

IC50: 0.122 μM (EGFR kinase), 0.078 μM (HER2 kinase), 0.585 μM (DHFR)[1]

In Vitro

EGFR/HER2-IN-6 (0-100 μM; 72 h) shows remarkable broad spectrum cytotoxic potency, and the cytotoxic potency against MCF7 cells is more potent than SOR[1].
EGFR/HER2-IN-6 (0-20 μM; 0-48 h) affects cell cycle and indeces apoptosis of MCF-7 cells[1].

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

Cell Cytotoxicity Assay[1]

Cell Line: HepG2 hepatocellular carcinoma, MCF7 breast cancer, HCT-116 colorectal carcinoma, PC-3 prostate, Hea cervical epithelioid carcinoma cell lines and WI-38 fetal lung fibroblast cells
Concentration: 0-100 μM
Incubation Time: 72 hours
Result: Exhibited cytotoxic potency to HepG2, MCF7, HCT-116, PC-3 and Hela cell lines with IC50s of 12.18, 2.37, 16.18, 18.39 and 9.43 μM. Showed a lower cytotoxic potency to WI-38 normal cell line with an IC50 value of 36.84 μM.

Apoptosis Analysis[1]

Cell Line: MCF-7 breast cancer cell line
Concentration: 0-20 μM
Incubation Time: 0-48 hours
Result: Through arrested cell cycle at G1/S and G1 phases and induced apoptosis in MCF-7 cells rather than necrosis to achieve anti-breast cancer activity.
In Vivo

EGFR/HER2-IN-6 (10 mg/kg; i.p. once per day for 20days) shows anti-breast cancer activity in mice[1].

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

Animal Model: 8-week-old swiss albino female mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection; 10 mg/kg once per day; for 20 days
Result: Decreased tumor volume 65.3% and reduced body weight 7.4% after 20 days of treatment.
Molecular Weight

387.46

Formula

C18H21N5O3S

SMILES

O=C(C1=CSC2=NC(CN3CCOCC3)=C(C4=CC=C(OC)C=C4)N21)NN

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
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EGFR/HER2-IN-6
Cat. No.:
HY-151156
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