On August 31, 2016, Miller, Michael L.; Fishkin, Nathan E.; Li, Wei; Whiteman, Kathleen R.; Kovtun, Yelena; Reid, Emily E.; Archer, Katie E.; Maloney, Erin K.; Audette, Charlene A.; Mayo, Michele F.; Wilhelm, Alan; Modafferi, Holly A.; Singh, Rajeeva; Pinkas, Jan; Goldmacher, Victor; Lambert, John M.; Chari, Ravi V. J. published an article.Safety of H-Idc-OH The title of the article was A New Class of Antibody-Drug Conjugates with Potent DNA Alkylating Activity. And the article contained the following:
The promise of tumor-selective delivery of cytotoxic agents in the form of antibody-drug conjugates (ADC) has now been realized, evidenced by the approval of two ADCs, both of which incorporate highly cytotoxic tubulin-interacting agents, for cancer therapy. An ongoing challenge remains in identifying potent agents with alternative mechanisms of cell killing that can provide ADCs with high therapeutic indexes and favorable tolerability. Here, we describe the development of a new class of potent DNA alkylating agents that meets these objectives. Through chem. design, we changed the mechanism of action of our novel DNA crosslinking agent to a monofunctional DNA alkylator. This modification, coupled with linker optimization, generated ADCs that were well tolerated in mice and demonstrated robust antitumor activity in multiple tumor models at doses 1.5% to 3.5% of maximally tolerated levels. These properties underscore the considerable potential of these purpose-created, unique DNA-interacting conjugates for broadening the clin. application of ADC technol. Mol Cancer Ther; 15(8); 1870-8. æ¼?016 AACR. The experimental process involved the reaction of H-Idc-OH(cas: 79815-20-6).Safety of H-Idc-OH
The Article related to antibody drug conjugate dna alkylating antitumor activity, Immunochemistry: Antibodies and Immunoglobulins and other aspects.Safety of H-Idc-OH
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Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles