EGFR/HER2-IN-4

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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.

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

EGFR/HER2-IN-4 Chemical Structure

CAS No. : 1879071-89-2

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Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target^[1]

EGFR

0.6 nM (IC₅₀)

HER2

Cellular Effect

Cell Line	Type	Value	Description	References
A-431	IC₅₀	1.52 nM Compound: 1d	Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by CCK8 assay	[PMID: 30600209]
HCC827	IC₅₀	0.31 nM Compound: 1d	Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay Antiproliferative activity against human HCC827 cells harboring EGFR L858R mutant after 72 hrs by CCK8 assay	[PMID: 30600209]
MDA-MB-453	IC₅₀	0.62 nM Compound: 1d	Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by CCK8 assay Antiproliferative activity against human MDA-MB-453 cells after 72 hrs by CCK8 assay	[PMID: 30600209]
NCI-H1975	IC₅₀	12.2 nM Compound: 1d	Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant after 72 hrs by CCK8 assay Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant after 72 hrs by CCK8 assay	[PMID: 30600209]

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.

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 T_max	4 h
C_max	92.32 μg/L
AUC_0-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.

1879071-89-2

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

Handling Instructions (2659 KB)

References

[1]. Debasis Das, et.al. In vivo efficacy studies of novel quinazoline derivatives as irreversible dual EGFR/HER2 inhibitors, in lung cancer xenografts (NCI-H1975) mice models. Bioorg Chem. 2020 Jun;99:103790. [Content Brief]

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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