LAQ824 (NVP-LAQ824,Dacinostat) (Synonyms: Dacinostat, NVP-LAQ824)

Cell lines

Dexamethasone –sensitive human multiple myeloma (Dex-sensitive MM.1S) cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

20 nM 24-, 48-, or 72-hour

Applications

As an inhibitor of HDAC, LAQ824 induces apoptosis in multiple myeloma cell lines resistant to conventional therapies. In this experiment, Dex or LAQ824 alone produced only 15% and 7% growth inhibition, respectively, but produced 51% inhibition when used in combination.

Animal models

Female BALB/c mice administered 32D.p210 leukemic cells via tail vein injection

Dosage form

The mice were given intraperitoneal injection of either 25 mg/kg LAQ824 or D5W vehicle on a daily basis, beginning 3 days after introduction of the leukemic cells.

Applications

Treatment of mice with LAQ824 delayed the onset of symptoms of leukemia and lethality as compared to mice treated with the vehicle control. Median survival times were 20 days in the LAQ824-treated mice and 15.5 days in the vehicle control mice.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Catley L, Weisberg E, Tai Y T, et al. NVP-LAQ824 is a potent novel histone deacetylase inhibitor with significant activity against multiple myeloma. Blood, 2003, 102(7): 2615-2622.

[2] Weisberg E, Catley L, Kujawa J, et al. Histone deacetylase inhibitor NVP-LAQ824 has significant activity against myeloid leukemia cells in vitro and in vivo. Leukemia, 2004, 18(12): 1951-1963.