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CAS No. : 219989-84-1
MCE 国际站:Ixabepilone
产品活性:Ixabepilone (BMS-247550) 是一种可口服的 microtubule抑制剂,能够与微管蛋白结合,促进微管蛋白的聚合和微管的稳定,因此使细胞停滞在 G2-M 期,诱导细胞凋亡。
研究领域:Cell Cycle/DNA Damage | Cytoskeleton | Apoptosis | Anti-infection
作用靶点:Microtubule/Tubulin | Apoptosis | Bacterial
In Vitro: BMS-247550 is a highly potent cytotoxic agent capable of killing cancer cells at low nanomolar concentrations and retains its antineoplastic activity against human cancers that are naturally insensitive to paclitaxel or that have developed resistance to paclitaxel.
In Vivo: BMS-247550 demonstrates antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumors. BMS-247550 is more efficacious than paclitaxel in all five paclitaxel-resistant tumors evaluated in this study (four human and one murine): the clinically derived paclitaxel resistant Pat-7 ovarian carcinoma, the A2780Tax ovarian carcinoma that is resistant to paclitaxel because of tubulin mutations, the HCT116/VM46 MDR colon carcinoma, the clinically derived paclitaxel-resistant Pat-21 breast carcinoma, and the murine fibrosarcoma M5076. Against three paclitaxel-sensitive human tumor xenografts, BMS-247550 produces antitumor activity equivalent to paclitaxel: A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma.
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