Ixabepilone

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Chemical Structure| 219989-84-1 同义名 : BMS-247550;Aza-epothilone B;Azaepothilone BBMS 2475501. Trade name: Ixempra.
CAS号 : 219989-84-1
货号 : A131078
分子式 : C27H42N2O5S
纯度 : 99%+
分子量 : 506.698
MDL号 : MFCD04307791
存储条件：

Pure form Sealed in dry,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(167.75 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

2% DMSO+30% PEG 300+2% Tween 80+water 7 mg/mL

生物活性
描述 Ixabepilone is an epothilone analogue that shows cytotoxic potency against tumor cell lines with IC50 values ranging from 1.4 to 34.5 nM. The in vitro IC90 values of ixabepilone in HCT116, HCT/VM46, A2780S, and A2780Tax cells were 7.3, 16, 6.9 and 12 nM, respectively. Ixabepilone potently induced tubulin polymerization with an EC0.01 value of 3.5 μM. Eight-hour exposure of 7.5 nM ixabepilone almost completely blocked HCT116 cells in mitosis[1]. Ixabepilone inhibited cell viability in triple negative breast cancer cell lines with the IC50 values of 10 nM for MDA-MB-231 cells and 8 nM for SUM159 cells. After 72-hour incubation with 5 nM ixabepilone, the mammosphere formation in MDA-MB-231 and SUM159 cells were 0.21% and 0.30%, respectively. In immunocompromised nude rats implanted with Pat-7 tumor, i.v. administration of ixabepilone (3 mg/kg per injection) on a schedule of every 8 days × 2 elicited more than 5 log cell kill, and 4 of 6 cures. In A2780Tax human ovarian carcinoma xenograft, Iiabepilone (6.3 mg/kg per injection) on a schedule of every 2 days × 5 produced 2.5 log cell kill. In a paclitaxel-sensitive tumor model implanted with LS174T human colon carcinoma, ixabepilone (16 mg/kg per injection) administrated every 4 days × 3 yielded 2.3 log cell kill[2].
作用机制 The cellular cytotoxic activities of ixabepilone are linked to the induction of tubulin polymerization and the blockage of cell cycle progression in cancer cells[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.97mL

0.39mL

0.20mL

9.87mL

1.97mL

0.99mL

19.74mL

3.95mL

1.97mL
参考文献

[1]Lee FY, Borzilleri R, et al. BMS-247550: a novel epothilone analog with a mode of action similar to paclitaxel but possessing superior antitumor efficacy. Clin Cancer Res. 2001;7(5):1429-37.

[2]Tanei T, Choi DS, et al. Antitumor activity of Cetuximab in combination with Ixabepilone on triple negative breast cancer stem cells. Breast Cancer Res. 2016;18(1):6.

[3]Lee FY, Borzilleri R, et al. Preclinical discovery of ixabepilone, a highly active antineoplastic agent. Cancer Chemother Pharmacol. 2008 Dec;63(1):157-66.

[4]BMS2475501

[5]Peterson JK, Tucker C, et al. In vivo evaluation of ixabepilone (BMS247550), a novel epothilone B derivative, against pediatric cancer models. Clin Cancer Res. 2005 Oct 1;11(19 Pt 1):6950-8.