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编 号:F756153
分子式:C14H11BrN4O2S
分子量:379.23
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生物活性:
EGFR/HER2/DHFR-IN-1 is a potent anticancer agent with high selectivity against MCF-7 breast cancer cells. EGFR/HER2/DHFR-IN-1 is a multiple inhibitor of EGFR/HER2 kinase and DHFR, with IC50s of 0.153 μM, 0.108 μM, 0.291 μM, respectively. EGFR/HER2/DHFR-IN-1 arrests cell cycle at G1/S and induces cells apoptosis.

体内研究:
Caspase-3 is a lysosomal enzyme involved in apoptosis, and is used as a biomarker for detection of apoptotic cells.EGFR/HER2-IN-7 (compound 39) (10 mg/kg; i.p.; once daily; 20 d) shows anti-breast cancer activity in vivo and increases caspase-3 immunoexpression in brease cancer mice.Animal Model:Breast cancer with non-lactating mammary glands animal model in Swiss albino female mice (8-weeks-old)
Dosage:10 mg/kg
Administration:Intraperitoneal injection; once daily; 20 days
Result:Inhibited tumor volume with reduction rate of 76.5%.Reduced body weight with loss rate of 17.4%.Showed the Caspase-3 score of 1.33.

体外研究:
EGFR/HER2-IN-7 (compound 39) shows remarkable broad spectrum cytotoxic potency, with an IC50 value of 1.83 μM against MCF-7 breast cancer cell lines.EGFR/HER2-IN-7 (1.83 μM) induces cell apoptosis by arreating cell cycle at G1/S.
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