Novel antibody drug conjugates containing exatecan derivative-based cytotoxic payloads

Bioorganic and Medicinal Chemistry Letters

Volumn 26, Issue 6, 2016, Pages 1542-1545

  Nakada, Takashi ^a   Masuda, Takeshi ^a   Naito, Hiroyuki ^a   Yoshida, Masao ^a   Ashida, Shinji ^a   Morita, Koji ^a   Miyazaki, Hideki ^a   Kasuya, Yuji ^a   Ogitani, Yusuke ^a   Yamaguchi, Junko ^a   Abe, Yuki ^a   Honda, Takeshi ^a  

^a DAIICHI SANKYO CO   (Japan)

Author keywords

Anti HER2; Antibody drug conjugate; Camptothecin; Cancer therapy; Cytotoxic payload; Exatecan; Linker; Oncology; Trastuzumab

Indexed keywords

AMIDE; ANTIBODY CONJUGATE; CARBENE; CYTOTOXIC AGENT; EPIDERMAL GROWTH FACTOR RECEPTOR 2; EXATECAN; EXATECAN ANTIBODY CONJUGATE; LYSOSOME ENZYME; TRASTUZUMAB; UNCLASSIFIED DRUG; ANTINEOPLASTIC AGENT; CAMPTOTHECIN; MONOCLONAL ANTIBODY;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTIPROLIFERATIVE ACTIVITY; ARTICLE; CANCER CELL LINE; CONTROLLED STUDY; DRUG CONJUGATION; DRUG CYTOTOXICITY; DRUG EFFICACY; DRUG POTENCY; DRUG RELEASE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; HYDROPHILICITY; HYDROPHOBICITY; IN VITRO STUDY; INTERNALIZATION; MOUSE; NONHUMAN; PHYSICAL CHEMISTRY; STEREOSPECIFICITY; ANALOGS AND DERIVATIVES; ANIMAL; CELL PROLIFERATION; CELL SURVIVAL; CHEMISTRY; CONFORMATION; DISEASE MODEL; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; FEMALE; INTRACEREBROVENTRICULAR DRUG ADMINISTRATION; MAMMARY NEOPLASMS, EXPERIMENTAL; METABOLISM; PATHOLOGY; STRUCTURE ACTIVITY RELATION; TUMOR CELL LINE;

ANIMALS; ANTIBODIES, MONOCLONAL, HUMANIZED; ANTINEOPLASTIC AGENTS; CAMPTOTHECIN; CELL LINE, TUMOR; CELL PROLIFERATION; CELL SURVIVAL; DISEASE MODELS, ANIMAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG SCREENING ASSAYS, ANTITUMOR; FEMALE; HUMANS; INJECTIONS, INTRAVENTRICULAR; MAMMARY NEOPLASMS, EXPERIMENTAL; MICE; MOLECULAR CONFORMATION; STRUCTURE-ACTIVITY RELATIONSHIP; TRASTUZUMAB;

EID: 84998996835     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2016.02.020     Document Type: Article

References (8)

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4. +.
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6. 6 DAR was calculated by UV absorption measurement of 280 nm and 370 nm.
7. 7 Aggregation rate was measured by high performance liquid chromatography (HPLC). Column; Tosoh TSK gel G3000SWXL (300 × 7.8 mm). Mobile phase; 0.5 mL/min 0.03 M phosphate buffer (0.2 M arginine, pH 6.8). Sample; 10 μL (1 mg/mL) injection; ADC (1) in phosphate buffered saline (pH 7.5), ADC (2), (7a), and (7b) in acetate buffer red 5% sorbitol (pH 5.5), and ADC (3)–(6) in phosphate buffered saline (pH 6.0).
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