| Identification | Back Directory | [Name]
Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- | [CAS]
2319587-80-7 | [Synonyms]
Anticancer agent 82
Cinnoline, 8-chloro-4-[4-(3-chloro-5-methoxyphenyl)-1-piperazinyl]- | [Molecular Formula]
C19H18Cl2N4O | [MOL File]
2319587-80-7.mol | [Molecular Weight]
389.28 |
| Chemical Properties | Back Directory | [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 |
| Hazard Information | Back Directory | [Uses]
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[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 |
| [storage]
Store at -20°C | [References]
[1] Martínez-Pe?a 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 |
|
|