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
- Purity & Documentation
- References
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All EGFR Isoforms
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Biological Activity
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EGFRL858R/T790M 12 nM (IC50) |
EGFRC797S 13 nM (IC50) |
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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
|
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
|
[PMID: 31749909] |
| Sf21 | IC50 |
>1000 nM
Compound: 3
|
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
|
[PMID: 31749909] |
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.
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.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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