Vinflunine Inhibitor

Solid. Powder

98.00%

Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent

816.93

DMSO: Soluble
(<1mg/ refers to the product slightly soluble or insoluble)

C45H54F2N4O8

CC[C@@]1(C=CCN2CC3)[C@@]2([H])[C@@]3(C(C=C([C@](C4=C5C(C=CC=C6)=C6N4)(CC(C[C@@H](C(F)(F)C)C7)([H])CN7C5)C(OC)=O)C(OC)=C8)=C8N9C)[C@]9([H])[C@](C(OC)=O)(O)[C@@H]1OC(C)=O

162652-95-1

Effects of Vinflunine on L1210 cell proliferation are determined using a standard growth inhibition assay. Exponentially growing L1210 cells (1.5 × 105cells/well) in a 24-well plate are exposed to a range of concentrations of test compounds for 48 hours, prior to determining cell numbers using an electronic particle counter based on linear interpolation between data points.(Only for Reference)

Determination of Microtubule Polymer Mass: Purified tubulin (17 uM) is polymerized into microtubules in the abence or presence of a range of vnflunine concentrations (35 minutes; 37 degree C) in 75mM PIPES, 1.8mM MgCl2, 1.0mM EGTA, and 1.5mM GTP (pH 6.8) using sea urchin (Strongylocentrotus purpuratus) axonemes as seeds for assembly initiation. After incubation, polymerized microtubules are separated from unpolymerized tubulin by centrifugation (150,000 × g; 1 hour; 35 degree C). The supernatant is aspirated, the sedimented microtubules are depolymerized in assembly buffer by incubation on ice (2 hours), and the protein content is determined.

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 5mg/kg, with no effect at 0.63mg/kg (P > 0.05). An ID50 value (dose which inhibits 50% of bFGF-induced neovascularisation) is calculated as 1mg/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 0.16mg/kg Vinflunine, although maximal overall inhibition is reached at the maximal tolerated dose (MTD) of 20mg/kg. [5]