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.
- CAS No.: 1879071-97-2
- Formula: C30H33ClN6O4
- Molecular Weight:577.07
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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EGFR 0.6 nM (IC50) |
HER2 0.6 nM (IC50) |
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.
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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 hour
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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.
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:99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg
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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
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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.
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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-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%
Chemical Information
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CAS No. 1879071-97-2
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Molecular Weight 577.07
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Formula C30H33ClN6O4
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR/HER2-IN-5 Related Classifications
HY-147994 Related Classifications
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