Rosabulin (STA 5312) (STA 5312) 是一种有效且具有口服活性的微管抑制剂，可抑制微管组装。 Rosabulin (STA 5312) 具有广谱抗肿瘤活性。
Rosabulin is a potent microtubule inhibitor, with anti-cancer activities.
Rosabulin demonstrates substantial anti-proliferative activity against a wide range of cancer cell linesin vitro, with IC50 values extending down into the nanomolar range. Rosabulin is inhibition of microtubule assembly and subsequent arrest of the cell cycle. Rosabulin is active against several tumor cell lines that express moderate to high levels of P-glycoprotein (Pgp), including lines insensitive to Taxol, Vincristine, and Adriamycin in which Pgp activity is a major contributor to the MDR phenotype[1].
Rosabulin has shown in vivo activity in several murine tumors as well as human tumor xenograft models, including drug resistant tumors[1].
[1]. Keizo Koya, et al. STA-5312, a novel tubulin inhibitor, demonstrates the anti-cancer activity against chemotherapy-resistant cancers. Proc Amer Assoc Cancer Res, Volume 45, 2004
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