Anagrelide (hydrochloride) | 盐酸阿那格雷

MCE 国际站：Anagrelide (hydrochloride)

中文名：盐酸阿那格雷

CAS：58579-51-4

品牌：MedChemExpress (MCE)

存储条件：4°C, sealed storage, away from moisture

生物活性：Anagrelide hydrochloride (BL4162A) 是一种用于治疗原发性血小板增多症的药物。目标：PDE Anagrelide hydrochloride 是一种口服咪唑并喹唑啉药物，已被证明可以降低血小板计数升高和各种骨髓增生性疾病 (MPD) 血小板增多症患者的血栓形成风险。它目前被 FDA 批准用于治疗原发性血小板增多症 (ET) 和与真性红细胞增多症 (PV) 相关的血小板增多症。已知阿那格雷抑制血小板环磷酸腺苷 (cAMP) 磷酸二酯酶的浓度超过用于治疗 ET 的剂量。阿那格雷在肝脏中广泛代谢，其代谢物主要通过尿液排泄[1]。阿那格雷是一种公认的降血小板药物。研究还调查了阿那格雷对血小板的影响，表明血小板功能与 ET 中的血小板计数一样重要 [2]。

体外：Anagrelide hydrochloride (BL4162A) 有效抑制骨髓巨核细胞的发育 (IC50=26 nM)[1]。 Anagrelide (0.05、0.3、1 µM；12 天) hydrochloride 仅抑制巨核细胞生长，不抑制非巨核细胞生长[2]。 Anagrelide (0.1-10000 nM) hydrochloride 在 GIST882 细胞系中诱导细胞毒性作用[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内：Anagrelide hydrochloride (BL4162A; 5 mg/kg/bid；持续 10 天) 抑制或减少 GIST2B、GIST9、GIST882 模型中的肿瘤生长[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Adult female athymic mice bearing GIST2B, GIST3, GIST9, GIST882 model[3] Dosage: 5 mg/kg Administration: Twice daily; for 10 days Result: Inhibited or reduced tumor growth in three (GIST2B, GIST9, GIST882) of these four models. Clinical Trial

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研究领域：Metabolic Enzyme/Protease  |  Apoptosis

作用靶点：Phosphodiesterase (PDE)  |  Apoptosis

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参考文献：[1]. Pescatore, S.L. and C. Lindley, Anagrelide: a novel agent for the treatment of myeloproliferative disorders. Expert Opin Pharmacother, 2000. 1(3): p. 537-46.

[2]. Petrides, P.E., Anagrelide: what was new in 2004 and 2005? Semin Thromb Hemost, 2006. 32(4 Pt 2): p. 399-408.