A PDE3 inhibitor
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Labeled Version(s)
33280Anagrelide-13C3
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Anagrelide (hydrochloride)

Item No. 21411

Technical Information
Formal Name
6,7-dichloro-1,5-dihydro-imidazo[2,1-b]quinazolin-2(3H)-one, monohydrochloride
CAS Number
58579-51-4
Synonyms
  • BL 4162A
  • BMY 26538-01
Molecular Formula
C10H7Cl2N3O • HCl
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 0.25 mg/mlDMSO: 2 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
216, 257 nm
SMILES
ClC1=C(CN(C2)C(N3)=NC2=O)C3=CC=C1Cl.Cl
InChi Code
InChI=1S/C10H7Cl2N3O.ClH/c11-6-1-2-7-5(9(6)12)3-15-4-8(16)14-10(15)13-7;/h1-2H,3-4H2,(H,13,14,16);1H
InChi Key
TVWRQCIPWUCNMI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Anagrelide is an inhibitor of phosphodiesterase 3 (PDE3; IC50 = 36 nM for the human platelet enzyme).1 It inhibits thrombopoietin-induced megakaryocytopoiesis of isolated human CD34+ progenitor cells (IC50 = 26 nM).2 Anagrelide reduces platelet aggregation induced by ADP, collagen, thrombin, or arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607) in isolated rabbit platelet rich-plasma (EC50s = 0.31, 0.08, 0.18, and 0.1 µg/ml, respectively).3 It inhibits platelet thrombus formation in a dog model of electrically induced carotid artery thrombosis when administered at doses ranging from 0.5 to 5 mg/kg.4 Formulations containing anagrelide have been used in the treatment of thrombocythemia.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, G., Franklin, R., Hong, Y., et alComparison of the biological activities of anagrelide and its major metabolites in haematopoietic cell cultures. Br. J. Pharmacol. 146(3), 324-332 (2005).

    2. Hong, Y., Wang, G., Gutierrez del Arroyo, A., et alComparison between anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: Selectivity of anagrelide for the megakaryocytic lineage. Leukemia 20(6), 1117-1122 (2006).

    3. Fleming, J.S., and Buyniski, J.P. A potent new inhibitor of platelet aggregation and experimental thrombosis, anagrelide (BL-4162A). Thromb. Res. 15(3-4), 373-388 (1979).

    4. Fleming, J.S., and Buyniski, J.P. Anagrelide. New drugs annual: Cardiovascular drugs 277-294 (1983).