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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
EGFRL858R/T790M 0.101 μM (IC50) |
EGFRL858R 0.477 μM (IC50) |
EGFRWT 1.771 μM (IC50) |
Cellular Effect
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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] |
In Vitro
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. Further protocols information, click here.
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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
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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