Anagrelide - CAS 68475-42-3
Catalog number: 68475-42-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C10H7Cl2N3O
Molecular Weight:
256.09
COA:
Inquire
Targets:
Phosphodiesterase (PDE)
Description:
Anagrelide is a phosphodiesterase inhibitor with antiplatelet activity with IC50 value of 36 nM for inhibition of phosphodiesterase 3. It inhibits the maturation of megakaryocytes into platelets, reducing both megakaryocyte hyperproliferation and differentiation. It is antithrombocythemic used for the treatment of overproduction of blood platelets. It is a synthetic quinazoline derivative and is used as is a platelet-reducing agent. It reduces platelet production through a decrease in megakaryocyte maturation. It inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. It is a drug used for the treatment of essential thrombocytosis or overproduction of blood platelets. It also has been used in the treatment of chronic myeloid leukemia. It was developed by Shire and has been listed.
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Purity:
98%
Appearance:
Ivory powder
Synonyms:
6,7-Dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one;6-Chloro-1,2,3,5-tetrahydro iMidazo [2,1-b]quinazolin-2-one;Agrelin;Agrylin;Xagrid;Shire;Thromboreductin
Solubility:
Soluble in DMSO, not in water
Storage:
-20°C Freezer
MSDS:
Inquire
Application:
Anagrelide is used for the treatment of overproduction of blood platelets. It is a drug used for the treatment of essential thrombocytosis or overproduction of blood platelets. It also has been used in the treatment of chronic myeloid leukemia.
Quality Standard:
In-house standard
Quantity:
Kilograms to Tons
Boiling Point:
376.5°C at 760 mmHg
Melting Point:
280 °C
Density:
1.77±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
OTBXOEAOVRKTNQ-UHFFFAOYSA-N
InChI:
InChI=1S/C10H7Cl2N3O/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)
Canonical SMILES:
C1C2=C(C=CC(=C2Cl)Cl)NC3=NC(=O)CN31
Current Developer:
Anagrelide was developed by Shire and has been listed.
1.Blast transformation and fibrotic progression in polycythemia vera and essential thrombocythemia: a literature review of incidence and risk factors.
Cerquozzi S1, Tefferi A1. Blood Cancer J. 2015 Nov 13;5:e366. doi: 10.1038/bcj.2015.95.
Polycythemia vera (PV) and essential thrombocythemia (ET) constitute two of the three BCR-ABL1-negative myeloproliferative neoplasms and are characterized by relatively long median survivals (approximately 14 and 20 years, respectively). Potentially fatal disease complications in PV and ET include disease transformation into myelofibrosis (MF) or acute myeloid leukemia (AML). The range of reported frequencies for post-PV MF were 4.9-6% at 10 years and 6-14% at 15 years and for post-ET MF were 0.8-4.9% at 10 years and 4-11% at 15 years. The corresponding figures for post-PV AML were 2.3-14.4% at 10 years and 5.5-18.7% at 15 years and for post-ET AML were 0.7-3% at 10 years and 2.1-5.3% at 15 years. Risk factors cited for post-PV MF include advanced age, leukocytosis, reticulin fibrosis, splenomegaly and JAK2V617F allele burden and for post-ET MF include advanced age, leukocytosis, anemia, reticulin fibrosis, absence of JAK2V617F, use of anagrelide and presence of ASXL1 mutation.
2.Influence of platelet and white blood cell counts on major thrombosis - Analysis from a patient registry in Essential Thrombocythemia.
Buxhofer-Ausch V1,2, Steurer M3, Sormann S4, Schloegl E5, Schimetta W6, Gisslinger B1, Ruckser R7, Gastl G3, Gisslinger H1. Eur J Haematol. 2016 Apr 1. doi: 10.1111/ejh.12759. [Epub ahead of print]
OBJECTIVES: Although guidelines recommend normalization of platelet counts as an appropriate endpoint for treatment in high-risk essential thrombocythemia (ET), retrospective studies could not prove a correlation of diagnostic platelet counts with an increased thrombotic rate. There is, however, an increasing evidence that leukocytosis is an important risk factor for arterial thrombosis in myeloproliferative neoplasms.
3.Contemporary approach to essential thrombocythemia and polycythemia vera.
Aruch D1, Mascarenhas J. Curr Opin Hematol. 2016 Mar;23(2):150-60. doi: 10.1097/MOH.0000000000000216.
PURPOSE OF REVIEW: Management of polycythemia vera and essential thrombocythemia requires understanding of the key concepts regarding diagnosis, risk stratification, and management.
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CAS 68475-42-3 Anagrelide

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