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Ifosfamide

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Chemical Structure| 3778-73-2 同义名 : Isophosphamide;NSC109724;Ifosfamidum.;Ifex;US brand names: Cyfos;Naxamide;Isoendoxan;iphosphamide;Iphosphamid;Ifomide
CAS号 : 3778-73-2
货号 : A205362
分子式 : C7H15Cl2N2O2P
纯度 : 98%
分子量 : 261.09
MDL号 : MFCD00057374
存储条件:

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(191.51 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
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
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

[1]Johnstone EC, Lind MJ, et al. Ifosfamide metabolism and DNA damage in tumour and peripheral blood lymphocytes of breast cancer patients. Cancer Chemother Pharmacol. 2000;46(6):433-41.

[2]Chang TK, Yu L, et al. Enhanced cyclophosphamide and ifosfamide activation in primary human hepatocyte cultures: response to cytochrome P-450 inducers and autoinduction by oxazaphosphorines. Cancer Res. 1997 May 15;57(10):1946-54.

[3]Helal M. Prenatal effects of transplacental exposure to ifosfamide in rats. Biotech Histochem. 2016 Jul;91(5):357-68

[4]Karle P, Renner M, et al. Necrotic, rather than apoptotic, cell death caused by cytochrome P450-activated ifosfamide. Cancer Gene Ther. 2001 Mar;8(3):220-30

[5]Vredenburg G, den Braver-Sewradj S, et al. Activation of the anticancer drugs cyclophosphamide and ifosfamide by cytochrome P450 BM3 mutants. Toxicol Lett. 2015 Jan 5;232(1):182-92