EGFR-IN-77
EGFR-IN-77 (Compound 4a) is a selective EGFRT790M/L858R inhibitor, with an IC50 of 0.101 μM against EGFRT790M/L858R, 0.477 μM against EGFRL858R, and 1.771 μM against wild-type EGFR. EGFR-IN-77 exerts selective antiproliferative effects on EGFRT790M/L858R non-small cell lung cancer. EGFR-IN-77 can be used for the research of EGFRL858R/T790M double-mutant non-small cell lung cancer.
For research use only. We do not sell to patients.
- CAS No.: 2222930-49-4
- Formula: C26H28N6O3
- Molecular Weight:472.54
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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
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All EGFR Isoforms
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Biological Activity
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EGFRL858R/T790M 0.101 μM (IC50) |
EGFRL858R 0.477 μM (IC50) |
EGFRWT 1.771 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| NCI-H1975 | IC50 |
0.184 μM
Compound: 4a
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Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31581004] |
| NCI-H292 | IC50 |
8.321 μM
Compound: 4a
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Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31581004] |
| PC-9 | IC50 |
0.137 μM
Compound: 4a
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Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
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[PMID: 31581004] |
EGFR-IN-77 inhibits purified TL double mutant EGFR kinase with an IC50 of 0.101 μM, L858R mutant EGFR kinase with an IC50 of 0.477 μM, and WT EGFR kinase with an IC50 of 1.771 μM, exhibiting 17.52-fold selectivity for TL EGFR over WT EGFR[1].
EGFR-IN-77 inhibits proliferation of H1975 (TL EGFR) NSCLC cells with an IC50 of 0.184 μM, PC9 (L858R EGFR) cells with an IC50 of 0.137 μM, and H292 (WT EGFR) cells with an IC50 of 8.321 μM, exhibiting 45.27-fold selectivity for H1975 cells over H292 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2222930-49-4
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Molecular Weight 472.54
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Formula C26H28N6O3
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SMILES
O=C(NC1=CC(NC2=NC(C3=CN(C)C4=C3C=CC=C4)=CC=N2)=C(C=C1N(CCO)C)OC)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-IN-77 Related Classifications
HY-153605 Related Classifications
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