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pomalidomide basic information |
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 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 |
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. |