2375107-27-8
2375107-27-8 structure
- Name: Mutated EGFR-IN-3
- Chemical Name: Mutated EGFR-IN-3
- CAS Number: 2375107-27-8
- Molecular Formula: C31H29FN4O2
- Molecular Weight: 508.59
- Catalog: Signaling Pathways JAK/STAT Signaling EGFR
- Create Date: 2020-04-16 11:18:53
- Modify Date: 2024-01-12 13:58:39
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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].
| Name | Mutated EGFR-IN-3 |
|---|
| 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 |