Mutated EGFR-IN-3
Modify Date: 2025-08-27 15:39:08
Mutated EGFR-IN-3 structure
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Common Name | Mutated EGFR-IN-3 | ||
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| CAS Number | 2375107-27-8 | Molecular Weight | 508.59 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C31H29FN4O2 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of Mutated EGFR-IN-3Mutated 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[1]. |
| Name | Mutated EGFR-IN-3 |
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| Description | 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[1]. |
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| Related Catalog | |
| Target |
EGFRL858R/T790M:12 nM (IC50) EGFRC797S:13 nM (IC50) |
| 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]. |
| References |
| Molecular Formula | C31H29FN4O2 |
|---|---|
| Molecular Weight | 508.59 |
| InChIKey | ZPNTXOKOIHPCLI-UHFFFAOYSA-N |
| SMILES | CN1CCN(c2ccc(Oc3ccc4c(c3)C(=O)N(Cc3ccccc3)c3cc(F)ccc3N4)cc2)CC1 |