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Anagrelide HCl

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Chemical Structure| 58579-51-4 同义名 : BL4162A;Anagrelide (hydrochloride);Thromboreductin;GALE-401;Xagrid;Agrylin;BMY 26538-01;Anagrelide hydrochloride
CAS号 : 58579-51-4
货号 : A139945
分子式 : C10H8Cl3N3O
纯度 : 99%+
分子量 : 292.549
MDL号 : MFCD01720337
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 6 mg/mL(20.51 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：

IP 2% DMSO+water 0.06 mg/mL clear

PO 0.5% CMC-Na 54 mg/mL suspension

生物活性
靶点

  • PDE
描述 Anagrelide Hydrochloride is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia), or overproduction of blood platelets, and also has been used in the treatment of chronic myeloid leukemia. It inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation[3]. Anagrelide was effective in patients with ET which had similar hematologic remission rate to hydroxyurea and could take effect more quickly than hydroxyurea[4]. Only at anagrelide concentrations of 10 to 500 times therapeutic doses did anagrelide inhibit megakaryocyte colony development: an anagrelide concentration of 5 micrograms/mL reduced colony numbers by 57% and colony size by 31%. Therapeutic concentrations of anagrelide influence primarily the postmitotic phase of megakaryocyte development, decreasing platelet production by reducing megakaryocyte size and ploidy, as well as by disrupting full megakaryocyte maturation[5]. In addition, food/caffeine delayed absorption of anagrelide. Anagrelide was generally well tolerated and had small effects on ECG (electrocardiogram) parameters and heart rate[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00306202 Leukemia Phase 1 Active, not recruiting October 4, 2022 Austria ... 展开 >> Local Institution Vienna, Austria, 1090 France Local Institution Nantes, France, 44093 Local Institution Paris Cedex 10, France, 75475 Local Institution Paris Cedex 12, France, 75571 Germany Local Institution Berlin, Germany, 13353 Local Institution Frankfurt, Germany, 60590 Local Institution Hannover, Germany, 30625 Italy Local Institution Monza (mi), Italy, 20052 Netherlands Local Institution Rotterdam, Netherlands, 3015 GJ United Kingdom Local Institution Manchester, Greater Manchester, United Kingdom, M27 4HA Local Institution Bristol, Somerset, United Kingdom, BS2 8BJ Local Institution Sutton, Surrey, United Kingdom, SM2 5PT Local Institution Birmingham, West Midlands, United Kingdom, B4 6NH 收起 <<
NCT01243944 Polycythemia Vera Phase 3 Completed - -
NCT00481052 Chronic Myeloid Leukemia Phase 2 Active, not recruiting December 2018 Italy ... 展开 >> Dipartimento Area Medica P.O. Ascoli Piceno, Italy, 63100 Unità Operativa Ematologica - Università degli Studi di Bari Bari, Italy, 70124 Ospedali Riuniti Bergamo, Italy, 24100 stituto di Ematologia "Lorenzo e A. Seragnoli" - Università degli Studi di Bologna - Policlinico S. Orsola - Malpighi Bologna, Italy Sezione di Ematologia e Trapianti Spedali Civili Brescia, Italy, 21125 Azienda Spedali Civili Brescia, Italy, 25100 ASL N.8 - Ospedale "A. Businco" - Struttura Complessa di Ematologia e CTMO Cagliari, Italy Ospedale Ferrarotto Catania, Italy, 95124 Azienda Ospedaliera Pugliese Ciaccio Catanzaro, Italy, 88100 Sezione di Ematologia e Fisiopatologia delle Emostasi - Azienda Ospedaliera - Arcispedale S. Anna Ferrara, Italy Azienda Ospedaliera Universitaria - Università degli Studi di Napoli "Federico II" - Facoltà di Medicina e Chirurgia Napoli, Italy Ospedale S. Luigi Gonzaga Orbassano, Italy, 10043 La Maddalena Casa di Cura di Alta Specialità Dipartimento Oncologico di III Livello Palermo, Italy Unità Operativa Ematologia e Centro Trapianti - Dipartimento di Oncologia ed Ematologia - AUSL Ospedale di Piacenza Piacenza, Italy Ospedale S.Maria delle Croci Ravenna, Italy, 48100 Calabria Dipartimento Emato-Oncologia A.O."Bianchi-Melacrino-Morelli" Reggio Calabria, Italy Università La Cattolica del Sacro Cuore Roma, Italy, 00168 Complesso Ospedaliero S. Giovanni Addolorata Roma, Italy, 00184 Università degli Studi "Sapienza" - Dip Biotecnologie Cellulari ed Ematologia - Divisione di Ematologia Roma, Italy U.O. Ematologia, Azienda Ospedaliera Universitaria Senese Siena, Italy, 53100 Policlinico Universitario - Clinica Ematologia Udine, Italy, 33100 Policlinico G.B. Rossi Verona, Italy, 37134 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.09mL

3.42mL

1.71mL

34.18mL

6.84mL

3.42mL
参考文献

[1]Tefferi A, Silverstein MN, 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.

[2]Silverstein MN, Petitt RM, et al. Anagrelide: a new drug for treating thrombocytosis. N Engl J Med. 1988 May 19;318(20):1292-4.

[3]Pescatore SL, Lindley C. Anagrelide: a novel agent for the treatment of myeloproliferative disorders. Expert Opin Pharmacother. 2000 Mar;1(3):537-46

[4]Ge X, Yang L, Jin J, Qian W, Li J, Yang R, Cao X, Jiang B, Wang Z, Hou M, Zhang W, Xiao Z, Zhao Y, Gao D, Zhang X, Wang S, Sun A, Fu J, Su L, Li K. [Efficacy and safety of anagrelide in treatment of essential thrombocythemia: multicenter, randomized controlled clinical trial]. Zhonghua Xue Ye Xue Za Zhi. 2015 Jul;36(7):547-52. Chinese

[5]Mazur EM, Rosmarin AG, Sohl PA, Newton JL, Narendran A. Analysis of the mechanism of anagrelide-induced thrombocytopenia in humans. Blood. 1992 Apr 15;79(8):1931-7

[6]Martínez-Sellés M, Datino T, Figueiras-Graillet L, Gama JG, Jones C, Franklin R, Fernández-Avilés F. Cardiovascular safety of anagrelide in healthy subjects: effects of caffeine and food intake on pharmacokinetics and adverse reactions. Clin Drug Investig. 2013 Jan;33(1):45-54