~(153)Sm标记平阳霉素偶联物

Conjugated Bleomycin A5-DTPA and Its Labeling With ~(153)Sm

  • 摘要: 进行了二乙三胺五乙酸酸酐 (c DTPAA)平阳霉素偶联后的 153 Sm标记。研究了平阳霉素与c DTPAA的偶联条件、偶联物化学计量组成, 探讨了 153 Sm与偶联物的络合条件及络合物的稳定性。在弱碱性介质中, 当 c DTPAA与平阳霉素的摩尔比大于 10时, 平阳霉素的偶联率可达 80 %;当摩尔比大于 15时, 偶联物的平均化学计量组成为平阳霉素与 DTPA的摩尔比为 1∶ 2;在 p H7~ 9体系中, 偶联物与 153 Sm摩尔比大于 8,室温反应 30 min,标记率可达 98%;标记物较稳定, 生理 p H下 6d内放化纯度大于 96 %。

     

    Abstract: Bleomycin A5(BLMA5) is conjugated with cyclic DTPA anhydride and labeled with 153 Sm. The conditions of conjugation and labeling are investigated. The possible composition of BLMA5-DTPA is analyzed by measurement and computation. The results show that bleomycin A5 can conjugate with DTPA anhydride easily when the mole ratio of cDTPAA to BLMA5 is more than 10 in weak basic media, and the conjugating yield is more than 80%;A molecule of BLMA5 conjugate with 2 molecule of cDTPAA when the mole ratio of cDTPAA to BLMA5 is not less than 15, and the conjugative positions is on 2 different N atoms. The results of labeling experiments indicate that the labeling yield of 153 Sm-DTPAA-BLMA5 is 98% at pH7~9 and room temperature for 30 min when the mole ratio of DTPA-BLMA5 to 153 Sm is more than 8 153 Sm-BLMA5-DTPA is stable and the radiochemical purity is more than 96% at room temperature for 6 days.

     

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