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编 号:F752061
分子式:C28H28D5N7O2
分子量:504.64
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生物活性:
Dosimertinib-d3-d3 is a potent and orally active EGFR inhibitor. Dosimertinib-d3-d3 decreases the expression of p-EGFR and p-ERK protein levels. Dosimertinib-d3-d3 shows antiproliferative and anti-tumor activity. Dosimertinib-d3-d3 has the potential for the research of non-small-cell lung cancer (NSCLC).

体内研究:
Dosimertinib (0.75、1.5、3 mg/kg;口服,每天一次,持续 24 天) 在小鼠体内显示出抗肿瘤活性。Animal Model:18-20 g, BALB/c nude mice (H1975 mouse xenograft model)
Dosage:0.75, 1.5, 3 mg/kg
Administration:Oral gavage; daily for 24 days
Result:Significantly reduced tumor size with tumor growth inhibition (TGI) of 72.94% and 97.62% at 1.5, 3 mg/kg, respectively.

体外研究:
Dosimertinib (compound 2h) (1, 10, 100, 100 nM; 2h) 以剂量依赖性方式降低 p-EGFR 和 p-ERK 蛋白水平。
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