Lenssen U, Hohorst H J
J Cancer Res Clin Oncol. 1979 Feb 19;93(2):161-4. doi: 10.1007/BF00406573.
The uptake of tritiated N,N-bis(2-chloroethyl)-diamido-phosphoric-acid into Ehrlich-Ascites-Tumor cells of mice was studied by means of the siliconoil-filtration technique. At 10 mM concentration no permeation of the metabolite into the tumor cells could be found within 5 min at 1 degrees C, while its congenors cyclophosphamide and 4-hydroperoxycyclophosphamide (1 mM) were shown to permeate into the cells very easily reaching saturation values. Thus lack of permeation into tumor cells of N,N-bis(2-chloroethyl)-diamidophosphoric-acid seems to be the reason for the poor cytotoxic activity of this metabolite of cyclophosphamide.
采用硅油过滤技术研究了氚标记的N，N-双（2-氯乙基）-二氨基磷酸进入小鼠艾氏腹水癌细胞的情况。在10 mM浓度下，在1℃时5分钟内未发现该代谢产物渗透进入肿瘤细胞，而其同类物环磷酰胺和4-氢过氧环磷酰胺（1 mM）很容易渗透进入细胞并达到饱和值。因此，N，N-双（2-氯乙基）-二氨基磷酸缺乏渗透进入肿瘤细胞的情况似乎是环磷酰胺这种代谢产物细胞毒性活性较差的原因。
