Treosulfan CAS# 299-75-2 曲奥舒凡

Treosulfan, a bifunctional alkylating agent and prodrug of a diepoxybutane derivative, shows potent cytotoxicity in vitro across various tumor cell lines. In leukemia and lymphoma cell models (e.g., HL-60, K562), treosulfan induces dose-dependent cytotoxicity with IC₅₀ values typically ranging from 50 to 200 µM, associated with DNA crosslinking and apoptosis. In vivo, treosulfan demonstrates strong antitumor activity in murine models of leukemia and ovarian carcinoma. In L1210 leukemia-bearing mice, treosulfan (400 mg/kg × 3 days, i.p.) significantly increased survival and produced marked tumor regression. In xenograft models of ovarian cancer (A2780), treosulfan (500 mg/kg, i.v.) reduced tumor volume by >70% compared with control, with lower systemic toxicity than busulfan or cyclophosphamide. Its well-tolerated myeloablative effect supports its preclinical use as a conditioning agent before hematopoietic stem cell transplantation.