| 产品描述: | Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type III intermediate filament protein vimentin (VIM), to induce hyperphosphorylation of Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability and pharmacokinetic profiles than FiVe1. |
| 体外研究: |
Vimentin-IN-1 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1[1]. Pharmacokinetic properties of Vimentin-IN-1 in mice[1] |
| 体内研究: |
Vimentin-IN-1 (compound 4e) (0-10 mM; 72 h) inhibits a marked improvement in potency with an IC50 value of 44 nM against HT-1080 fibrosarcoma, better than than FiVe1 (IC50=1.6 μM, HT-1080).
Vimentin-IN-1 (0.1 μM; 24 h) induces phosphorylation of VIM at Ser56.
Vimentin-IN-1 (100 μM; sampled at 0, 5, 15, 30, 45, and 60 min) exhibits poor stability with 0.0% remaining after 60 min of incubation in mouse liver microsome. |
| 保存条件: |
-80°C 6个月;-20°C 1个月 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.569 ml |
12.844 ml |
25.688 ml |
| 5 mM |
0.514 ml |
2.569 ml |
5.138 ml |
| 10 mM |
0.257 ml |
1.284 ml |
2.569 ml |
| 50 mM |
0.051 ml |
0.257 ml |
0.514 ml |
|
| 注意: |
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