1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR/HER2-IN-5

EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research.

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

EGFR/HER2-IN-5 Chemical Structure

EGFR/HER2-IN-5 Chemical Structure

CAS No. : 1879071-97-2

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  
Synthetic products have potential research and development risk.

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research[1].

IC50 & Target

EGFR

0.6 nM (IC50)

HER2

0.6 nM (IC50)

In Vitro

EGFR/HER2-IN-5 (compound 6h) (0-10 μM, 72 hours) shows good anti-proliferative activity against lung cancer, where the effect against mutant lung cancer HCC 827 is superior to that of NCI-H1975 and A431[1].

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

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 hour
Result: Inhibited NCI-H1975 cells, HCC 827 cells, A431 cells with the IC50values of 60.6 nM, 1.2 nM and 288.3 nM respectively.
In Vivo

EGFR/HER2-IN-5 (compound 6h) (oral gavage; 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg; every other day or every day; 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: 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg
Administration: Oral gavage; 99.5 mg/kg and 24.9 mg/kg for every other day for 25 days; 6.2 mg/kg for every day for 25 days
Result: Inhibited 84.11% of tumor xenografts growth at 99.5 mg/kg, 65.72% at 24.9 mg/kg, and 47% at 6.2 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-5 (compound 6h) oral (10 mg/kg)
Parameter
Oral Tmax 8 h
Cmax 39.4 μg/L
AUC0-a 780 μg/L*h
IV 5 mg/kg
half life 4.9 h
oral bioavailability 28.8%
Molecular Weight

577.07

Formula

C30H33ClN6O4

CAS No.
SMILES

O=C(NC1=CC2=C(NC3=CC=C(OCC4=NC=CC=C4)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
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

EGFR/HER2-IN-5 Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
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.

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
EGFR/HER2-IN-5
Cat. No.:
HY-147994
Quantity:
MCE Japan Authorized Agent: