Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- manufacturers
|
| | Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- Basic information |
| | Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- Chemical Properties |
| Boiling point | 606.3±65.0 °C(Predicted) | | density | 1.363±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | form | Solid | | pka | 5.56±0.10(Predicted) | | color | Light yellow to orange |
| | Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- Usage And Synthesis |
| Uses | Vimentin-IN-1 is a FiVe1 derivative, an orally active and selective anticancer agent. FiVe1 binds type IIIintermediate filament proteinvimentin(VIM), to induce hyperphosphorylationof Ser56, resulting selective disruption of mitosis and multinucleation in transformed VIM-expressing mesenchymal cancer cells. Vimentin-IN-1 shows better oral bioavailability andpharmacokineticprofiles than FiVe1[1]. | | in vivo | 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]
| Route | Dose (mg/kg) | AUC0-last (ng·h/mL) | AUC0-inf (ng·h/mL) | T1/2 (h) | Tmax (h) | Tlast (h) | Cmax (ng/mL) | | 4e | PO | 10 | 371.33 | 534.33 | 4.68 | 0.67 | 8 | 154.67 | | 4e | IP | 1 | 208.33 | 211.33 | 0.59 | 0.25 | 4 | 197.00 | | Five1 | PO | 25 | 309.78 | 339.21 | 4.57 | 0.5 | 18 | 110.43 |
| | References | [1] Martínez-Pea F, et al. Synthesis and biological evaluation of novel FiVe1 derivatives as potent and selective agents for the treatment of mesenchymal cancers. Eur J Med Chem. 2022 Nov 15;242:114638. DOI:10.1016/j.ejmech.2022.114638 |
| | Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- Preparation Products And Raw materials |
|