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Anagrelide

CAS No. : 68475-42-3

產品活性：Anagrelide, an inhibitor of phosphodiesterase type III (PDEIII) (IC₅₀=36?nM), inhibits platelet production. Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide plays in the antithrombopoietic action. The platelet-lowering agent.

研究領域：Metabolic Enzyme/Protease

作用靶點：Phosphodiesterase (PDE)

In Vitro: Anagrelide potently inhibits the development of marrow megakaryocytes (IC₅₀=26?nM).
Anagrelide is a distinct pharmacological agent that inhibit bone marrow megakaryocytopoiesis. Anagrelide (0.05, 0.3, 1 µM) inhibits only megakaryocytic cell growth not non-megakaryocytic cells. Anagrelide shifts cell growth to the non-megakaryocytic compartment, an effect that suggested that it was devoid of cytotoxic activity.
Anagrelide induces a cytotoxic effect in the GIST882 cell line at a submicromolar concentration (IC₅₀= 16 nM), but Anagrelide is only weakly active in the GIST48 cell line.Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro.

In Vivo: Anagrelide is effective in a GIST xenograft mouse model with KIT exon 9 mutation that may pose a therapeutic challenge, as these GISTs require a high daily dose of Imatinib.Anagrelide inhibits GIST growth in patient-derived mouse xenograft models. Anagrelide has therapeutic value in the treatment of GIST.Anagrelide has antitumoral activity in GIST xenograft models. Anagrelide (5 mg/kg/bid) inhibits or reduces tumor growth in GIST2B, GIST9, GIST882 model models.

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