EGFR-IN-165
EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFRL858R/T790M and EGFRWT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.
For research use only. We do not sell to patients.
- Formula: C26H21N5O5
- Molecular Weight:483.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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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
EGFR-IN-165 (Compound 4b) (0-5 μM, 48 h) effectively inhibits EGFR phosphorylation in a concentration-dependent manner in A431 cells and NCI-H1975 cells[1].
EGFR-IN-165 (1.25-10 μM, 24 h) effectively inhibits the migration of A431 cells at a concentration of 10 μM[1].
EGFR-IN-165 (2.5-20 μM, 48 h) reaches 12.91% apoptosis rate in NCI-H1975 cells at a concentration of 20 μM[1].
EGFR-IN-165 (2.5-20 μM, 24-48 h) induces cell cycle arrest in the G1 phase of NCI-H1975 cells[1].
EGFR-IN-165 has superior stability with a half-life of 38.5 h in human plasma and a low clearance rate in liver microsomes with an intrinsic clearance rate of 24.3 mL/min/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A431 and NCI-H1975 cells
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Concentration:0, 1.25, 2.5, 5 μM
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Incubation Time:48 h
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Result:Demonstrated significant and concentration-dependent inhibition of EGFR phosphorylation in A431 cells.
Exhibited effective and concentration-dependent inhibition of EGFR phosphorylation.
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Cell Line:A431 cells
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Concentration:1.25, 2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Effectively inhibited the migration at a concentration of 10 μM.
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Cell Line:NCI-H1975 cells
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Concentration:2.5, 5, 10 and 20 μM
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Incubation Time:48 h
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Result:Reached 12.91% apoptosis rate in NCI-H1975 cells at a concentration of 20 μM.
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Cell Line:NCI-H1975 cells
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Concentration:2.5, 5, 10 and 20 μM
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Incubation Time:24-48 h
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Result:The proportion of the G1 phase increased to 73.09 %, while the S phase decreased to 17.29 % and the G2 phase to 9.48 %.
Chemical Information
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Molecular Weight 483.48
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Formula C26H21N5O5
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SMILES
COC1=C(C=C2C(N=CN=C2NC3=CC=C(C(C)=C3)C(OC4=NN=C(O4)C5=CC=CC=C5)=O)=C1)OC
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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-IN-165 Related Classifications
HY-175011 Related Classifications
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