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编 号:F469986
分子式:C10H10Cl3N3O2
分子量:310.56
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生物活性:
Anagrelide hydrochloride monohydrate is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36?nM). Anagrelide hydrochloride monohydrate, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride monohydrate inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride monohydrate decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride monohydrate is a platelet-lowering agent and plays in the antithrombopoietic action.

体内研究:
Anagrelide (5 mg/kg/bid;持续 10 天) hydrochloride monohydrate 抑制或减少 GIST2B、GIST9、GIST882 模型中的肿瘤生长。Animal Model:Adult female athymic mice bearing GIST2B, GIST3, GIST9, GIST882 model
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.

体外研究:
Anagrelide hydrochloride monohydrate 有效抑制骨髓巨核细胞的发育 (IC50=26?nM)。Anagrelide(0.05、0.3、1 μM;12 天) hydrochloride monohydrate 仅抑制巨核细胞生长,不抑制非巨核细胞生长。Anagrelide (0.1-10000 nM) hydrochloride monohydrate 在 GIST882 细胞系中诱导细胞毒性作用。
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