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Cryptophycin-8 was prepared by the conversion of the epoxide group on cryptophycin-1 to a chlorohydrin. In the studies reported here, cryptophycin-8 was evaluated for preclinical activity against subcutaneous tumors of both mouse and human origin. At the highest non-toxic single course treatment, the following results were obtained (Table A). Cryptophycin-8 was less potent than cryptophycin-1 by approximately 4-fold; however, it was both more water soluble and had greater therapeutic efficacy, as demonstrated by % T/C, tumor cell log kill values, range of dose effectiveness and host cures.

Citation

T H Corbett, F A Valeriote, L Demchik, L Polin, C Panchapor, S Pugh, K White, J Knight, J Jones, L Jones, P LoRusso, B Foster, R A Wiegand, L Lisow, T Golakoti, C E Heltzel, J Ogino, G M Patterson, R E Moore. Preclinical anticancer activity of cryptophycin-8. Journal of experimental therapeutics & oncology. 1996 Mar;1(2):95-108

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PMID: 9414393

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