Mutated EGFR-IN-3
Mutated EGFR-IN-3 (compound 3) is a potent, ATP-competitive and highly selective allosteric dibenzodiazepinone inhibitor of the EGFR(L858R/T790M) and EGFR(L858R/T790M/C797S) mutants with IC50 values of 12 nM and 13 nM, respectively.
For research use only. We do not sell to patients.
- CAS No.: 2375107-27-8
- Formula: C31H29FN4O2
- Molecular Weight:508.59
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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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- Purity & Documentation
- References
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All EGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
EGFRL858R/T790M 12 nM (IC50) |
EGFRC797S 13 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Sf21 | IC50 |
11 nM
Compound: 3
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Inhibition of human N-terminal GST-tagged EGFR double T790M/L858R mutant (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
Inhibition of human N-terminal GST-tagged EGFR double T790M/L858R mutant (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
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[PMID: 31749909] |
| Sf21 | IC50 |
13 nM
Compound: 3
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Inhibition of human N-terminal GST-tagged EGFR triple T790M/L858R/C797S mutant (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
Inhibition of human N-terminal GST-tagged EGFR triple T790M/L858R/C797S mutant (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
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[PMID: 31749909] |
| Sf21 | IC50 |
154 nM
Compound: 3
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Inhibition of human N-terminal GST-tagged EGFR L858R mutant (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
Inhibition of human N-terminal GST-tagged EGFR L858R mutant (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
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[PMID: 31749909] |
| Sf21 | IC50 |
>1000 nM
Compound: 3
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Inhibition of human N-terminal GST-tagged EGFR (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
Inhibition of human N-terminal GST-tagged EGFR (696 to 1022 residues) expressed in Sf21 insect cells by HTRF assay
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[PMID: 31749909] |
In Vitro
Mutated EGFR-IN-3 inhibits EGFR through an allosteric mechanism, biochemical IC50 values at varying ATP concentrations: 10 µM, 10.0 µM, 100.0 µM, 1000.0 µM are 15 nM, 8.3nM,11.0 nM and 8.3 nM, respectively for L858R/T790M cells[1]. Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 7.0 µM, 3.3 µM, 3.8 µM, 4.0 µM and 4.5 µM for parental, WT, L858R, L858R/T790M and L858R/T790M/C797S, respectively in the absence of Cetuximab in Ba/F3 cells[1]. Mutated EGFR-IN-3 exhibits antiproliferative activities of a panel of EGFR allosteric inhibitors are 3.2 µM, 2.7 µM, 0.36 µM and 0.20 µM for WT,L858R, L858R/T790M and L858R/T790M/C797S, respectively in the presence of Cetuximab in Ba/F3 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. 2375107-27-8
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Molecular Weight 508.59
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Formula C31H29FN4O2
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SMILES
O=C1C2=CC(OC3=CC=C(N4CCN(C)CC4)C=C3)=CC=C2NC5=CC=C(F)C=C5N1CC6=CC=CC=C6
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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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Mutated EGFR-IN-3 Related Classifications
HY-130608 Related Classifications
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