产品
编 号：F751255
分子式：C19H18Cl2N4O
分子量：389.28
分子式：C19H18Cl2N4O
分子量：389.28
产品类型
规格
价格
是否有货
1mg
询价
询价
5mg
询价
询价
10mg
询价
询价
25mg
询价
询价
结构图
CAS No: 2319587-80-7
产品详情
生物活性：
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.
体内研究：
Vimentin-IN-1 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1.Pharmacokinetic properties of Vimentin-IN-1 in miceRouteDose (mg/kg)AUC0-last (ng·h/mL)AUC0-inf (ng·h/mL)T1/2 (h)Tmax (h)Tlast (h)Cmax (ng/mL)
4ePO10371.33534.334.680.678154.67
4eIP1208.33211.330.590.254197.00
Five1PO25309.78339.214.570.518110.43
体外研究：
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.
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.
体内研究：
Vimentin-IN-1 (compound 4e) (10 mg/kg; p.o.; single dose) shows better oral pharmacokinetic properties than Five1.Pharmacokinetic properties of Vimentin-IN-1 in miceRouteDose (mg/kg)AUC0-last (ng·h/mL)AUC0-inf (ng·h/mL)T1/2 (h)Tmax (h)Tlast (h)Cmax (ng/mL)
4ePO10371.33534.334.680.678154.67
4eIP1208.33211.330.590.254197.00
Five1PO25309.78339.214.570.518110.43
体外研究：
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.
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