Pomalidomide Basic information
Description In vitro In vivo
Product Name: Pomalidomide
Synonyms: 3-Amino-N-(2,6-dioxo-3-piperidyl)phthalimide;4-Amino-2-(2,6-dioxo-3-piperidyl)isoindoline-1,3-dione;Pomalidomide;Pomalidomide(CC-4047);ActiMid;CC-4047;4-AMino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione;1H-Isoindole-1,3(2H)-dione,4-aMino-2-(2,6-dioxo-3-piperidinyl)-
CAS: 19171-19-8
MF: C13H11N3O4
MW: 273.24
EINECS:
Product Categories: Inhibitor;CC-4047;Inhibitors
Mol File: 19171-19-8.mol
Pomalidomide Structure
Pomalidomide Chemical Properties
Melting point 318.5 - 320.5°
storage temp. 2-8°C
solubility DMSO: ≥14mg/mL
color yellow
Merck 14,135
Safety Information
RTECS NR3397905
MSDS Information
Pomalidomide Usage And Synthesis
Description Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM in PBMCs.
In vitro 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. Pomalidomide inhibits the growth of T regulatory cells which is stimulated by IL-2 with an IC50 of ~1 μM. Treatment with Pomalidomide (6.4 nM-10 μM) 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-γ 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 μM. Exposure of Raji cells to various concentrations of Pomalidomide (2.5-40 μg/mL) for 48 hours leads to a significant decrease in cell proliferation and DNA synthesis. There is a reduction of ~40% compared to vehicle-treated controls.
In vivo Pomalidomide enhances the antitumor effect of rituximab against B-cell lymphomas in severe combined immunodeficient mice. Administration of Pomalidomide in combination with rituximab, gives the mice a median survival period of 74 days compared with 58 days of CC5013/rituximab treatment and 45 days of rituximab nonotherapy. The synergistic effect of Pomalidomide and rituximab can be completely abrogated by depletion of NK cells, supporting the proposal that NK cell expansion is one mechanism by which Pomalidomide may augment rituximab antitumor activity.
Chemical Properties Yellow Solid
Uses Pomalidomide is a thalidomide derivative, a potent inhibitor of TNF-α production. It is an antiinflammatory and antitumor agent used in the treatment of multiple myeloma.
Uses Pomalidomide is a second generation immunomodulator, TNF-α inhibitor, and thalidomide analog. An inhibitor of LPS-induced TNFαrelease.
Uses Pomalidomide inhibits LPS-induced TNF-α release with IC50 of 13 nM
Definition ChEBI: An aromatic amine that is thalidomide substituted at position 4 on the isoindole ring system by an amino group. Used for the treatment of multiple myeloma in patients who failed to respond to previous therapies.
Pomalidomide Preparation Products And Raw materials