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.
CONJUGATE OF MONOMETHYL AURISTATIN F AND TRASTUZUMAB AND ITS USE FOR THE TREATMENT OF CANCER
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, (2017/05/15)
The present invention relates to an antibody-drug-conjugate or pharmaceutical composition comprising the same. From one aspect, the invention relates to an antibody-drug-conjugate (ADC) comprising an antibody consisting of the Trastuzumab or a biosimilar thereof, said antibody being conjugated to at least one drug consisting of a monomethyl auristatin F derivative. The invention also comprises method of treatment of cancer comprising administering to the subject an effective amount of said antibody-drug-conjugate or composition comprising the same.
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