Anagrelide
Anagrelide is an imidazoquinazoline anti-platelet compound that inhibits platelet aggregation at high doses and decreases platelet activity at low doses. Anagrelide inhibits phosphodiesterase III (PDE3). Anagrelide also decreases expression of GATA-1 and FOG1, suppressing megakaryocytopoiesis; it shows benefit in the treatment of chronic myeloproliferative disorders such as thrombocythemia. In vitro, anagrelide inhibits thombopoietin-mediated cell differentiation.
References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/18838646
Cas No. |
68475-42-3 |
---|---|
Purity |
≥98% |
Formula |
C10H7Cl2N3O |
Formula Wt. |
FW 256.09 |
Chemical Name |
6,7-dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one |
IUPAC Name |
6,7-dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one |
Melting Point |
280°C |
Appearance |
Almost White Crystal Powder |
Ahluwalia M, Donovan H, Singh N, et al. Anagrelide represses GATA-1 and FOG-1 expression without interfering with thrombopoietin receptor signal transduction. J Thromb Haemost. 2010 Oct;8(10):2252-61. PMID: 20586925.
McCarty JM, Melone PD, Simanis JP, et al. A preliminary investigation into the action of anagrelide: thrombopoietin-c-Mpl receptor interactions. Exp Hematol. 2006 Jan;34(1):87-96. PMID: 16413395.
Wang G, Franklin R, Hong Y, et al. Comparison of the biological activities of anagrelide and its major metabolites in haematopoietic cell cultures. Br J Pharmacol. 2005 Oct;146(3):324-32. PMID: 16041400.
Tefferi A, Silverstein MN, Petitt RM, et al. Anagrelide as a new platelet-lowering agent in essential thrombocythemia: mechanism of actin, efficacy, toxicity, current indications. Semin Thromb Hemost. 1997;23(4):379-83. PMID: 9263355.