1625677-63-5
1625677-63-5 structure
- Name: EGFR-IN-1
- Chemical Name: EGFR-IN-1
- CAS Number: 1625677-63-5
- Molecular Formula: C28H30N6O4
- Molecular Weight: 514.58
- Catalog: Signaling Pathways JAK/STAT Signaling EGFR
- Create Date: 2020-04-11 05:05:53
- Modify Date: 2025-08-27 13:07:45
-
EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1].
| Name | EGFR-IN-1 |
|---|
| Description | EGFR-IN-1 (compound 24) is an orally active and irreversible L858R/T790M mutant selective EGFR inhibitor. EGFR-IN-1 potently inhibits Gefitinib-resistant EGFR L858R, T790M with 100-fold selectivity over wild-type EGFR. EGFR-IN-1 displays strong antiproliferative activity against the H1975 cells and the first line mutant HCC827 cells. Antitumor activity[1]. |
|---|---|
| Related Catalog | |
| Target |
EGFRL858R/T790M |
| In Vitro | EGFR-IN-1 (10 μM; 72 hours) displays strong antiproliferative activity against the H1975 and HCC827 cells with IC50s of 4 and 28 nM, respectively[1]. EGFR-IN-1 inhibits p-EGFR in H1975 and HCC827 cells with IC50s of 4 and 9 nM, respectively. EGFR-IN-1 highly selective against a panel of 100 kinases[1]. Cell Proliferation Assay[1] Cell Line: NSCLC cell lines H1975 (T790M/L858R), HCC827 (∆746-750) Concentration: 10 μM Incubation Time: 72 hours Result: Inhibited H1975 nonsmall cell lung cancer cell line and the first line mutant HCC827 cell line with IC50s of 4 and 28 nM, respectively. |
| In Vivo | EGFR-IN-1 (30 mg/kg; p.o.; daily for 2 weeks) displays significant tumor growth inhibition with no observed loss in body weight[1]. EGFR-IN-1 evaluates in a time course PD experiment upon oral dosing at 30 mg/kg. EGFR-IN-1 shows a >50% inhibition of phosphorylation of EGFR for >12 h. EGFR-IN-1 reaches maximal concentration of 0.10 μM at 2 h and systemic exposure (AUC0-inf.) is 0.33 μM. h[1]. Animal Model: Female athymic nude mice (H1975 Tumor Xenograft)[1] Dosage: 30 mg/kg Administration: p.o.; daily for 2 weeks Result: Led to significant tumor growth inhibition with no observed loss in body weight. |
| References |
| Molecular Formula | C28H30N6O4 |
|---|---|
| Molecular Weight | 514.58 |