EGFR/HER2-IN-5 (化合物6h) 是一种具有口服活性的不可逆的双重抑制剂，其抑制EGFR活性IC50值为 0.6 nM。对 L858R 和 T790M 突变表现出有效的EGFR激酶抑制活性。 EGFR/HER2-IN-5 在体内具有强大的抗肿瘤功效，可以用于肺癌研究。

EGFR/HER2-IN-5 (compound 6h) is an orally active irreversible dual inhibitor. EGFR/HER2-IN-5 inhibits EGFR with an IC 50 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].

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 IC 50 values of 60.6 nM, 1.2 nM and 288.3 nM respectively.

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 (compound 6h) oral (10 mg/kg) Parameter Oral T max 8 h C max 39.4 μg/L AUC 0-a 780 μg/L*h IV 5 mg/kg half life 4.9 h oral bioavailability 28.8%

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