1879071-97-2
1879071-97-2 structure
- Name: EGFR/HER2-IN-5
- Chemical Name: EGFR/HER2-IN-5
- CAS Number: 1879071-97-2
- Molecular Formula: C30H33ClN6O4
- Molecular Weight: 577.07
- Catalog: Signaling Pathways JAK/STAT Signaling EGFR
- Create Date: 2022-08-28 11:02:04
- Modify Date: 2024-04-06 14:45:09
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EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research[1].
| Name | EGFR/HER2-IN-5 |
|---|
| Description | EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC50 value of 1.01 nM and demonstrates potent EGFR kinase inhibitory activities on L858R and T790M mutations. EGFR/HER2-IN-5 has potent antitumor efficacy in vivo and can be used for lung cancer research[1]. |
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| Related Catalog | |
| Target |
EGFR:0.6 nM (IC50) HER2:0.6 nM (IC50) |
| In Vitro | EGFR/HER2-IN-5 (compound 6h) (0-10 μM, 72 hours) shows good anti-proliferative activity against lung cancer, where the effect against mutant lung cancer HCC 827 is superior to that of NCI-H1975 and A431[1]. Cell Proliferation Assay[1] Cell Line: Human non-small cell lung cancer cell lines NCI-H1975 (T790M), HCC 827 (L858R), Human epithelial carcinoma cell lines A431 Concentration: 0-10 μM Incubation Time: 72 hour Result: Inhibited NCI-H1975 cells, HCC 827 cells, A431 cells with the IC50values of 60.6 nM, 1.2 nM and 288.3 nM respectively. |
| In Vivo | EGFR/HER2-IN-5 (compound 6h) (oral gavage; 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg; every other day or every day; 25 days) has good cancer suppression effect in a dose-dependent manner in the constructed NCI-H1975 tumor xenograft model[1]. Animal Model: BALB/c nude mice, female, 6–7 weeks of age with NCI-H1975 tumor xenograft[1] Dosage: 99.5 mg/kg, 24.9 mg/kg, 6.2 mg/kg Administration: Oral gavage; 99.5 mg/kg and 24.9 mg/kg for every other day for 25 days; 6.2 mg/kg for every day for 25 days Result: Inhibited 84.11% of tumor xenografts growth at 99.5 mg/kg, 65.72% at 24.9 mg/kg, and 47% at 6.2 mg/kg in nude mice. Animal Model: BALB/c nude mice, female, 6-7 weeks of age with NCI-H1975 tumor xenograft[1] Dosage: 10 mg/kg Administration: Oral gavage; 10 mg/kg; 25 days Result: The pharmacokinetic parameters of EGFR/HER2-IN-5 oral (10 mg/kg) Parameter Oral Tmax 8 h Cmax 39.4 μg/L AUC0-a 780 μg/L*h IV 5 mg/kg half life 4.9 h oral bioavailability 28.8% |
| References |
| Molecular Formula | C30H33ClN6O4 |
|---|---|
| Molecular Weight | 577.07 |