2413958-04-8
2413958-04-8 structure
- Name: EGFR kinase inhibitor 1
- Chemical Name: EGFR kinase inhibitor 1
- CAS Number: 2413958-04-8
- Molecular Formula: C30H31N7O2
- Molecular Weight: 521.61
- Catalog: Signaling Pathways Apoptosis Apoptosis
- Create Date: 2022-10-16 13:53:54
- Modify Date: 2025-10-08 15:17:43
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EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1].
| Name | EGFR kinase inhibitor 1 |
|---|
| Description | EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1]. |
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| Related Catalog | |
| Target |
EGFR (WT):37 nM (IC50) EGFRL858R/T790M:1.7 nM (IC50) EGFRL858R/T790M/C797S:>300 nM (IC50) |
| In Vitro | EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively[1]. EGFR kinase inhibitor 1 (0.05, 0.5, 5 µM; 48 h) induces apoptosis in a dose-dependent manner[1]. EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase[1]. EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells[1]. Cell Cytotoxicity Assay[1] Cell Line: A549, H1975 cells Concentration: Incubation Time: 72 h Result: Showed antiproliferation activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively. Apoptosis Analysis[1] Cell Line: H1975 cells Concentration: 0.05, 0.5, 5 µM Incubation Time: 48 h Result: Induced apoptosis in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: H1975 cells Concentration: 4, 20, 100 nM Incubation Time: 48 h Result: Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM. |
| References |
| Molecular Formula | C30H31N7O2 |
|---|---|
| Molecular Weight | 521.61 |