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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- CAS. Nr.: 1879071-89-2
- Formel: C24H27ClFN5O3
- Molecular Weight:487.95
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
EGFR 0.6 nM (IC50) |
HER2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-431 | IC50 |
1.52 nM
Compound: 1d
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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
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[PMID: 30600209] |
| HCC827 | IC50 |
0.31 nM
Compound: 1d
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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
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[PMID: 30600209] |
| MDA-MB-453 | IC50 |
0.62 nM
Compound: 1d
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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
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[PMID: 30600209] |
| NCI-H1975 | IC50 |
12.2 nM
Compound: 1d
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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
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[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. Further protocols information, click here.
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Cell Line:Human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R), Human epithelial carcinoma cell lines A431
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Concentration:0-10 μM
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Incubation Time:72 hours
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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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1]
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Dosage:81.4mg/kg, 20.4mg/kg, 5.1mg/kg
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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
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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.
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Animal Model:BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg; 25 days
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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%
Chemical Information
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CAS. Nr. 1879071-89-2
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Molecular Weight 487.95
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Formel C24H27ClFN5O3
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SMILES
O=C(NC1=CC2=C(NC3=CC=C(F)C(Cl)=C3)N=CN=C2C=C1OCCOCC)/C=C/CN(C)C
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
EGFR/HER2-IN-4 Related Classifications
HY-147992 Related Classifications
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