IPI-145 (INK1197)

Cell lines

Primary B cells and primary T 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.

Reacting condition

IC50 value : 0.5 or 9.5 nM

Applications

IPI-145 showed potent anti-proliferative activity against both primary B cells and primary T cells, with IC50 values of 0.5 nM and 9.5 nM, respectively. Thus, it inhibited neutrophil migration and basophil activation.

Animal models

Rats with previously established air pouches

Dosage form

1, 2.5, 5 and 10 mg/kg; p.o.

Applications

At the doses of 5 and 10 mg/kg, IPI-145 significantly inhibited neutrophil migration. More specifically, in the 10 mg/kg dose group, all animals showed significantly decreased neutrophil migration. In the 5 and 2.5 mg/kg dose groups, the results were more variable. The animals treated with 1 mg/kg IPI-145 showed little inhibition.

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]. Winkler DG1, Faia KL, DiNitto JP, Ali JA, White KF, Brophy EE, Pink MM, Proctor JL, Lussier J, Martin CM, Hoyt JG, Tillotson B, Murphy EL, Lim AR, Thomas BD, Macdougall JR, Ren P, Liu Y, Li LS, Jessen KA, Fritz CC, Dunbar JL, Porter JR, Rommel C, Palombella VJ, Changelian PS, Kutok JL. PI3K-δ and PI3K-γ inhibition by IPI-145 abrogates immune responses and suppresses activity in autoimmune and inflammatory disease models. Chem Biol. 2013 Nov 21;20(11):1364-74.