Abstract

Abstract A family of novel warheads derived from dolastatins or auristatins were designed and synthesized. They showed similar or better antitumor activities against several typical cancer cell lines compared with dolastatin 10 or monomethylauristatin E or F. The conjugated ADCs with Trastuzumab have showed potent activities against Her2 breast cancer cell lines. The validated platform with novel cytotoxins can be potentially used to ADCs discovery and development. Citation Format: Shanghui Hu, Lucy X. Zhao, Xu Liu, Chao Li, Wei Hu, Zunrong Wang, Xufang Tian. Building a powerful ADCs discovery and development platform with novel dolastatin/auristatin payloads. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 2646. doi:10.1158/1538-7445.AM2014-2646

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