Anagrelide

Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM) . Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action[1][2][3].

Product Specifications

CAS Number

[68475-42-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; Phosphodiesterase (PDE)

Type

Reference compound

Related Pathways

Apoptosis; Metabolic Enzyme/Protease

Applications

Cancer-programmed cell death

Field of Research

Cancer; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/anagrelide.html

Purity

99.87

Solubility

DMSO : 2.56 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1NC2=NC3=C(C(Cl)=C(Cl)C=C3)CN2C1

Molecular Formula

C10H7Cl2N3O

Molecular Weight

256.09

Precautions

H302, H315, H319, H335

References & Citations

[1]Guosu Wang, 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.|[2]Y Hong, et al. Comparison between Anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: selectivity of Anagrelide for the megakaryocytic lineage. Leukemia. 2006 Jun;20 (6) :1117-22.|[3]Olli-Pekka Pulkka, et al. Anagrelide for Gastrointestinal Stromal Tumor. Clin Cancer Res. 2019 Mar 1;25 (5) :1676-1687.