86-MM3919.00-0250 - pomalidomide | 19171-19-8

Pomalidomide

Pomalidomide

Pomalidomide (CC-4047) is an anti-angiogenic and immunomodulatory agent. Pomalidomide is a ligand for CRBN. Cost-effective and quality-assured.

<p>Applications 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.<br>References Ruchelman, A. et al.: Bioorg. Med. Chem. Lett., 23, 360 (2013); Latif, T. et al.: Exp. Hematol. Oncol., 1, 27 (2012); Man, H. et al.: Bioorg. Med. Chem. Lett., 13, 3415 (2003); Muller, G. et al.: Bioorg. Med. Chem. Lett., 9, 1625 (1999)<br></p>

<p>Pomalidomide is an immunomodulatory agent that inhibits transcriptional regulation by interacting with the pomalidomide-binding protein, which prevents its interaction with RNA polymerase II and thereby prevents DNA transcription. The study with U266 cells demonstrated that pomalidomide targets CRBN, part of an E3 ligase complex, and inhibits its autoubiquinitation and supresses a critical gene (IRF4, interferon regulatory factor 4) for myeloma cell growth with concentrations up to 10 μM.In vitro assays have shown that pomalidomide has inhibitory effects on cell signaling pathways, such as the NF-κB pathway. Pomalidomide also decreases the production of proinflammatory cytokines, such as TNFα and IL-1β, by inhibiting their synthesis or their release from activated monocytes. Recently, the promoting effect of pomalidomide, as its analog lenalidomide, on erythropoiesis (production of red blood cells) has been investigated, demonstrating positive results for its use as a potential new therapy agent for β-hemoglobinopathies.</p>