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Ixabepilone

CAS No. : 219989-84-1

MCE 國際站：Ixabepilone

產(chǎn)品活性：Ixabepilone (BMS-247550) 是一種可口服的 microtubule抑制劑，能夠與微管蛋白結(jié)合，促進微管蛋白的聚合和微管的穩(wěn)定，因此使細(xì)胞停滯在 G2-M 期，誘導(dǎo)細(xì)胞凋亡。

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Cytoskeleton  |  Apoptosis  |  Anti-infection

作用靶點：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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