DUPA(OtBu)-OH是一种DUPA前体。DUPA用作传递Docetaxel(DTX)的靶向基序，可用于治疗表达前列腺特异性膜抗原(PSMA)的前列腺肿瘤。
CAS：1026987-94-9
分子式：C23H40N2O9
分子量：488.57
纯度：98%
存储：Store at -20°C

Background:

DUPA(OtBu)-OH is a DUPA precursor. DUPA is used as the targeting moiety to actively deliver Docetaxel (DTX) for treatment of Prostate-Specific Membrane Antigen (PSMA) expressing prostate cancer.

DUPA(OtBu)-OH (DUPA precursor 17) is a 2-[3-(1,3-dicarboxypropyl)ureido]pentanedioic acid (DUPA) reagent[1]. The targeting ligand DUPA enhances the transport capability and selectivity of Paclitaxel (PTX) to tumor cells via prostate-specific membrane antigen (PSMA) mediated endocytosis. Besides, DUPA is conjugated with PTX via a disulfide bond, which facilitates the rapid and differential drug release in tumor cells[2].

DUPA-targeted Docetaxel (DTX) conjugate with longer spacer has no toxicity in major organs of treated mice[3].

[1]. Roy J, et al. DUPA conjugation of a cytotoxic indenoisoquinoline topoisomerase I inhibitor for selectiveprostate cancer cell targeting. J Med Chem. 2015 Apr 9;58(7):3094-103. [2]. Lv Q, et al. Prostate-Specific Membrane Antigen Targeted Therapy of Prostate Cancer Using a DUPA-Paclitaxel Conjugate. Mol Pharm. 2018 May 7;15(5):1842-1852. [3]. Peng ZH, et al. Spacer length impacts the efficacy of targeted docetaxel conjugates in prostate-specificmembrane antigen expressing prostate cancer. J Drug Target. 2013 Dec;21(10):968-80.