β-Glu-PAB (CH2NH2) -Exatecan (Compound 9a) is a topoisomerase I inhibitor. β-Glu-PAB (CH2NH2) -Exatecan binds to the topoisomerase I-DNA complex to prevent DNA strand reconnection, thereby inducing DNA breakage and cell apoptosis. β-Glu-PAB (CH2NH2) -Exatecan can be specifically cleaved by β-glucuronidase highly expressed in the tumor microenvironment to release Exatecan for cytotoxic effect. β-Glu-PAB (CH2NH2) -Exatecan is also an intermediate of Mal ((3S,3aR,6S,6aR) -hexahydrofuro [3, 2-B]furan-3,6-diamine-PEG12) -β -Glu-Pab-Exatecan. β-Glu-PAB (CH2NH2) -Exatecan is promising for research of cancers[1].