产品描述: | Ixabepilone (BMS-247550) is an orally bioavailable microtubule inhibitor, which binds to tubulin and promotes tubulin polymerization and microtubule stabilization, thereby arrests cells in the G2-M phase of the cell cycle and induces tumor cell apoptosis. |
靶点: |
Apoptosis;Microtubule Associated;Apoptosis; MicrotubuleAssociated |
体内研究: |
In vivo, BMS-247550 has clearly demonstrated antitumor activity that is superior to paclitaxel in both paclitaxel-resistant and -sensitive tumors. BMS-247550 is more efficacious compared to paclitaxel in all five paclitaxel-resistant tumors evaluated in this study (four human and one murine): i.e., 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: i.e., A2780 human ovarian carcinoma, HCT116, and LS174T human colon carcinoma |
细胞实验: |
HCT116 cells from cultures are collected by trypsinization after 1, 2, 4, 8, 16, and 24 h exposure to 7.5 nm of BMS-247550. Cells are pelleted and fixed in 80% ethanol at −20°C. After an overnight storage at −20°C, cells are rehydrated with PBS buffer and DNA stain by incubation with propidium iodide (5 μg/ml) in 0.1% RNase for 15–30 min. Fluorescence-activated cell sorter acquisition is performed using the FACS Calibur instrument and analysis is done using Cellquest and Modfit software. (Only for Reference) |
参考文献: |
1.Lee FY, et al. Clin Cancer Res. 2001, 7(5):1429-1437. |
溶解性: |
Ethanol:93 mg/mL (183.5 mM) DMSO:93 mg/mL (183.5 mM) H2O:<1 mg/mL |
保存条件: |
-20℃ |
配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
1 mM |
1.974 ml |
9.868 ml |
19.736 ml |
5 mM |
0.395 ml |
1.974 ml |
3.947 ml |
10 mM |
0.197 ml |
0.987 ml |
1.974 ml |
50 mM |
0.039 ml |
0.197 ml |
0.395 ml |
|
注意: |
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