For research purposes only

Cat. No BA94673140

Availability - up to 100 mg in stock
- larger amount can be synthesized in 6 weeks

Description of biological activity

Tubulin polymerization inhibitor. The compound is a tubulin polymerization inhibitor [US2005/14765 A1, 2005] with IC50 0.574 μmol. The polymerization of the tubulin into microtubules was monitored by turbidimetry as follows: the tubulin was adjusted to a concentration of 10 μm (1 mg/ml) in the RB/2 30percent glycerol buffer, to which were added 1 mM GTP and 6 mM MgCl2. The polymerization was initiated by increasing the temperature from 6 °C. to 37 °C in a cuvette with a 1 cm optical path length, placed in a UVIKON 931 spectrophotometer (Kontron) equipped with a thermostatically-regulated cuvette holder. The increase in turbidity of the solution was monitored at 350 nm. The compound was dissolved at 10 mM in DMSO and added at variable concentrations (0.5 to 10 μm) to the tubulin solution before polymerization. The IC50 was defined as the concentration of the product which inhibits the rate of polymerization by 50%.

Keywords: Anti-cancer

TECHNICAL INFORMATION

3-[4-(2-Trifluoromethyl-4-phenyl-1H-imidazol-5-ylcarbonyl)piperazin-1-yl]-benzonitrile tubulin polymerization inhibitor.

IUPAC Name: 3-[4-(2-Trifluoromethyl-4-phenyl-1H-imidazol-5-ylcarbonyl)piperazin-1-yl]-benzonitrile

CAS Number: 807623-93-4

Purity: > 96% chemical purity (LCMS)

1H-NMR spectrum (click to enlarge)

REFERENCES

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