Vinflunine (Tartrate)|cas 1201898-17-0|DC Chemicals

Vinflunine (Tartrate)|cas 1201898-17-0|DC Chemicals

Vinflunine Tartrat is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.

Target: Microtubule/Tubulin

The major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth duration, and a reduction in shortening duration.

Product Name: Vinflunine (Tartrate)|Cat No: DC9509|Cas: 1201898-17-0|Molecule Formular: C49H60F2N4O14|Molecule Weight: 967.0159|Other names: Vinflunine (Tartrate)

Vinflunine Tartrat is a new vinca alkaloid uniquely fluorinated with the properties of mitotic-arresting and tubulin-interacting activity.
The major effects of Vinflunine on dynamic instability are a slowing of the microtubule growth rate, an increase in growth duration, and a reduction in shortening duration. The effects of Vinflunine on the readmilling rate is examined by following [3H]GTP incorporation into MAP-rich microtubules, and the IC50 is 0.42 μM. Vinflunine induced mitotic accumulation with IC50 with 18.8 nM, which decreases the centromere dynamicity by 44% and increases the time centromeres spent ina paused state by 63%. Treatment of Vinflunine induces a rapid change in endothelial cell shape: cells retracts and assumes a rounded morphology. Mean IC50 values are 9.9 × 10-5 M × 10-5 M for fibronectin and 5.0× 10-5 M × 10-5 M for type IV collagen. A short 4 hours exposure of endothelial cells to Vinflunine at 10-8</SUP-10-4 M results in an inhibition of endothelial cell motility response to NIH3T3 cells-derived angiogenic factors. Inhibition is dose dependent, with a mean IC50 value of 7.1 × 10-7 × 10-7 M.
Intravenous treatment of mice with Vinflunine, immediately before and 2 day after Matrigel implantation, results in a dose-dependent inhibition of the bFGF-induced angiogenic response, compared with vehicle-treated animals. Inhibition of haemoglobin content is significant at 1.25, 2.5 and 5 mg/kg, with no effect at 0.63 mg/kg (P > 0.05). An ID50 value (dose which inhibits 50% of bFGF-induced neovascularisation) is calculated as 1 mg/kg. Low doses of Vinflunine reduce the number of experimental liver metastases by human LS174T colon cancer cell. A slight overall decrease in liver metastatic foci is already observed at the very low dose of 0.16 mg/kg Vinflunine, although maximal overall inhibition is reached at the maximal tolerated dose (MTD) of 20 mg/kg.

For research only, not for human use!