120205-52-9Relevant articles and documents
Synthesis and evaluation of novel dolastatin 10 derivatives for versatile conjugations
Yokosaka, Shinya,Izawa, Akiko,Sakai, Chizuka,Sakurada, Eri,Morita, Yasuhiro,Nishio, Yukihiro
, p. 1643 - 1652 (2018)
Dolastatin 10 (1) is a highly potent cytotoxic microtubule inhibitor (cytotoxicity IC50 5.0 nM) and several of its analogs have recently been used as payloads in antibody drug conjugates. Herein, we describe the design and synthesis of a series of novel dolastatin 10 analogs useful as payloads for conjugated drugs. We explored analogs containing functional groups at the thiazole moiety at the C-terminal of dolastatin 10. The functional groups included amines, alcohols, and thiols, which are representative structures used in known conjugated drugs. These novel analogs showed excellent potency in a tumor cell proliferation assay, and thus this series of dolastatin 10 analogs is suitable as versatile payloads in conjugated drugs. Insights into the structure–activity relationships of the analogs are also discussed.
REACTION MEDIUM CONTAINING WATER-SURFACTANT MIXTURE
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Page/Page column 14-15, (2017/11/01)
The present invention is directed to reaction mixtures comprising a water-surfactant mixture and a co-solvent. This technology reduced the amount of organic solvents needed for performing chemical reactions. Furthermore, compared to reaction mixtures lack
COMPOSITION FOR THE TREATMENT OF IGF-1R EXPRESSING CANCER
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Page/Page column 114, (2017/05/17)
The present invention relates to a method for the treatment of IGF-IR expressing cancers as well as to a compositions and a kit for said traitment. From one aspect, the invention reates to the combined use of a first antibody for the determination of the IGF-IR status of a cancer and a second antibody used as an ADC for the treatment of said cancer.