生物活性 | |||
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描述 | The DNA alkylator is irreversibly crosslinked with DNA strand, which interferes with DNA synthesis. Ifosfamide is an alkylating chemotherapeutic agent that exhibits activity against a wide range of tumors[3]. It was transformed into cytotoxic metabolites by enzymes in the liver. Ifosfamide is activated by the cytochrome P450 family. Ifosfamide inhibited the activity of CYP2B1 in C8III-1 cells at 0-5 mM. Only at high concentration (5 mM), Ifosfamide was cytotoxic to CrFK cells which did not express CYP2B1 [4]. The CYP-BM3 mutant activated ifosfamide, which inhibited U2OS cells[5]. Ifosfamide administration prior to mating resulted in an increased percentage of post-implantation loss and resorbed fetuses in pregnant rats treated with 50 mg/kg ifosfamide at day 18 of gestation compared to the control rats. But Ifosfamide causes no obvious difference with the control rats at 25 mg/kg [3]. | ||
作用机制 | Ifosfamide is a DNA alkylator that exhibits activity against a wide range of tumors by being transformed into cytotoxic metabolites. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
3.83mL 0.77mL 0.38mL |
19.15mL 3.83mL 1.92mL |
38.30mL 7.66mL 3.83mL |
参考文献 |
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