Ifosfamide是一种氮芥类烷化剂，其活性代谢物通过在 DNA 链间和链内形成交联，破坏 DNA 的复制和转录功能，从而抑制细胞增殖，常用于癌症研究。
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Type
HazMat fee for 500 gram (Estimated)
Excepted Quantity
USD 0.00
Limited Quantity
USD 15-60
Inaccessible (Haz class 6.1), Domestic
USD 80+
Inaccessible (Haz class 6.1), International
USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic
USD 100+
Accessible (Haz class 3, 4, 5 or 8), International
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.
Ifosfamide/异环磷酰胺 细胞实验
Cell Line
Concentration
Treated Time
Description
References
MCF-7 breast cancer cells
9.20 ± 2.01 mM
24 hours
To evaluate the antiproliferation activities of LEM-IFO and SAL-IFO on MCF-7 cells, the results showed that the IC50 of LEM-IFO and SAL-IFO were 0.200 ± 0.005 mM and 0.270 ± 0.025 mM, respectively, significantly lower than the IC50 of free IFO (9.20 ± 2.01 mM).
Sci Rep. 2019 Jan 24;9(1):695.
HeLa cervical cancer cells
7.69 ± 1.88 mM
24 hours
To evaluate the antiproliferation activities of LEM-IFO and SAL-IFO on HeLa cells, the results showed that the IC50 of LEM-IFO and SAL-IFO were 0.165 ± 0.025 mM and 0.141 ± 0.035 mM, respectively, significantly lower than the IC50 of free IFO (7.69 ± 1.88 mM).
Sci Rep. 2019 Jan 24;9(1):695.
HeLa cells
0.003, 0.03, 0.3, 30, 60 µg/mL
To evaluate the effect of BvRE on ifosfamide cytotoxicity, results showed that BvRE in combination with ifosfamide exhibited significant synergistic cytotoxic effects.
root extract on ifosfamide-induced in vivo toxicity and in vitro cytotoxicity. Sci Rep.
Ifosfamide/异环磷酰胺 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
C57BL/6 mice
Ifosfamide-induced hemorrhagic cystitis model
Intraperitoneal injection
400 mg/kg
Single dose, monitored for 6 hours
To investigate the pathological mechanisms of ifosfamide-induced hemorrhagic cystitis and the protective effects of IPSE. Results showed that IPSE pretreatment significantly alleviated inflammation, urothelial denudation, and edema induced by ifosfamide.
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