2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  3. EGFR
  4. EGFR/HER2-IN-4

EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research.

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EGFR/HER2-IN-4 Chemical Structure

EGFR/HER2-IN-4 Chemical Structure

CAS No. : 1879071-89-2

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EGFR/HER2-IN-4 Related Antibodies

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Description

EGFR/HER2-IN-4(compound 6d) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-4 inhibits EGFR with an IC50 value of 0.6 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-4 has potent antitumor efficacy in vivo and can be used for lung cancer research[1].

IC50 & Target[1]

EGFR

0.6 nM (IC50)

HER2

 

In Vitro

EGFR/HER2-IN-4 (compound 6d) (0-10 μM, 72 hours) shows well anti-proliferative activity against human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R) and human epithelial carcinoma cell lines A431[1].

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

EGFR/HER2-IN-4 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R), Human epithelial carcinoma cell lines A431
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Inhibited NCI-H1975 cells, HCC 827 cells, A431 cells with the IC50values of 107 nM,0.2 nM and 20 nM respectively.
In Vivo

EGFR/HER2-IN-4 (compound 6d) (orally gavage; 5.1-81.4 mg/kg; for 25 days) has good cancer suppression effect in a dose-dependent manner in the constructed NCI-H1975 tumor xenograft model[1].

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

Animal Model: BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1]
Dosage: 81.4mg/kg, 20.4mg/kg, 5.1mg/kg
Administration: Oral gavage; 81.4mg/kg and 20.4mg/kg for every other day for 25 days; 5.1mg/kg for every day for 25 days
Result: Inhibited 95.21% of tumor xenografts growth at 81.4mg/kg, 71.01% at 20.4 mg/kg, and 55.1% at 5.1 mg/kg in nude mice.
Animal Model: BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; 25 days
Result: The pharmacokinetic parameters of EGFR/HER2-IN-4 oral (10 mg/kg)
Parameter
Oral Tmax 4 h
Cmax 92.32 μg/L
AUC0-a 1030.9 μg/L*h
IV 5 mg/kg
half life 6.8 h
oral bioavailability 46.1%
Molecular Weight

487.95

Formula

C24H27ClFN5O3
CAS No.
SMILES

O=C(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OCCOCC)/C=C/CN(C)C
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/HER2-IN-4 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:

EGFR/HER2-IN-41879071-89-2EGFREpidermal growth factor receptorErbB-1HER1HER2Lung cancerNCI-H1975NSCLCXenograftInhibitorinhibitorinhibit

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