MC-Gly-Gly-Phe-Gly-GABA-Exatecan is an agent linker conjugate for ADC, with an inhibitor for Topoisomerase Exatecan with IC50 of 22 μM. MC-Gly-Gly-Phe-Gly-GABA-Exatecan targets various antibodies, exhibits cytotoxic and antitumor efficacy in vitro and in vivo.
MC-Gly-Gly-Phe-Gly-GABA-Exatecan (0-10 μM) exhibits cytotoxicity in cells SR (CD30 positive), HL60 (CD33 positive), U251 (CD70 positive) and Calu-6 (B7-H3 positive) through functions with CD30, CD33, CD70 and B7-H3[2].
MC-Gly-Gly-Phe-Gly-GABA-Exatecan (10 mg/kg, i.v. once a week for 2 weeks) exhibits antitumor efficacy in A375 xenograft mice[2].
References:
[1]. Hettmann T, et al., Anti-her3 antibody-drug conjugate. Patent WO2015155998 [2]. Ogitani Y, et al., Wide application of a novel topoisomerase I inhibitor-based drug conjugation technology. Bioorg Med Chem Lett. 2016 Oct 15;26(20):5069-5072.