Pomalidomide

2 years -80 in solvent

Injection i.p.

Raji, SU-DHL-4 and SU-DHL-10 cell lines

Dissolved in DMSO, final concentrations 2.5-40 ug/mL

Dissolved in DMSO to make a 10 mg/mL stock solution and diluted to a final concentration of 1 mg/mL in sterile 0.9% normal saline.

Pomalidomide inhibits lipopolysaccharide (LPS) stimulated TNF-alpha release in human PBMC and in human whole blood with IC50 values of 13 nM and 25 nM, respectively. [1] Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ca.1 uM. [2] Treatment with Pomalidomide (6.4 nM-10 uM) increases the production of IL-2 in human peripheral blood T cells, and is slightly more potent in the CD4+ subset than in the CD8+ subset. Pomalidomide is significantly more potent than CC-5013 at elevating IL-2, IL-5, and IL-10 levels, but only slightly more potent than CC-5013 at elevating IFN-gamma levels. Pomalidomide enhances, SEE and Raji cells induced AP-1 transcriptional activity in Jurkat cells in a dose-dependent manner, with a maximal enhancement of 4-fold at 1 uM. [3] Exposure of Raji cells to various concentrations of Pomalidomide, (2.5-40 ug/mL) for 48 hours leads to a significant decrease in cell proliferation and DNA synthesis., There is a reduction of, ca.40% compared to vehicle-treated controls. [4]

24 or 48 hours

For assessment of cell apoptosis, Lymphoma cell lines are exposed to Pomalidomide (5 ug/mL) for 24 hours or 48 hours. The cells are stained with FITC-labeled Annexin V and propidium iodine. Cell apoptosis is analyzed by multicolor flow cytometric analysis using a fluorescence-activated cell sorter/FACStar Plus flow cytometer. Cells are scored as apoptotic if they are Annexin V–positive and propidium iodine–negative/positive (early and late apoptosis, respectively). For determination of cell proliferation, the Lymphoma cell lines are exposed to Pomalidomide (2.5, 5, 10, 20, and 40 ug/mL) for 24 hours or 48 hours. 1 uCi per well (96-well plate) of [3H]-thymidine is added and cells are incubated for another 18 hours. Cells are then harvested using the Harvest system into the 96-well glass filters and [3H]-thymidine uptake is measured using an automated scintillation counter.

Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs. Pomalidomide can be utilized in PROTAC as a ligand for targeting E3 ligase and inhibiting the E3 ligase protein cereblon (CRBN). Pomalidomide promotes apoptosis and cell cycle arrest.

Pomalidomide is a derivative of thalidomide and up to 10, 000 times more potent than thalidomide.