Cell lines

CLL cell lines

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

24 h,48 h and 72 h; 1 μM.

Applications

Anti-IgM–supported CLL cell viability was reduced in the presence of PCI-32765 from 69% to 33% at 24 hours, and to 31% and 29% after 48 and 72 hours, respectively. Anti-IgM stimulation induced an average 27%±12% increase in viability after 24 hours compared with unstimulated controls. Preincubation with 1 μM PCI-32765 before anti-IgM stimulation significantly reduced CLL cell viability to 98%±8% of unstimulated controls. Survival signals from NLCs were also effectively inhibited by PCI-32765.

Animal models

CB17 SCID mice and Eμ-TCL1 transgenic (Tg) mice on a C3H/BL6 background

Dosage form

Suboptimal (2.5 mg/kg/d); optimal (25 mg/kg/d)

Applications

In the adoptive transfer TCL1 mouse model, animals treated PCI-32765 at 2 weeks post cell transfer with the suboptimal (2.5 mg/kg/d) and optimal (25 mg/kg/d) doses exhibited a transient lymphocytosis at day 4, with an average of 7- and 10-fold increases in circulating TCL1 leukemia cells, respectively.

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] Ponader S, Chen S S, Buggy J J, et al. The Bruton tyrosine kinase inhibitor PCI-32765 thwarts chronic lymphocytic leukemia cell survival and tissue homing in vitro and in vivo[J]. Blood, 2012, 119(5): 1182-1189.