Anagrelide

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Anagrelide 

Anagrelide是一种III型磷酸二酯酶（PDEIII）抑制剂 (IC50=36 nM)，抑制血小板生成。Anagrelide 是一种咪唑喹唑啉衍生物，可作为血小板聚集抑制剂。Anagrelide 具有抗血栓形成作用。

Anagrelide

Anagrelide Chemical Structure

CAS No. : 68475-42-3

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Anagrelide 的其他形式现货产品:

Anagrelide hydrochloride

生物活性

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[1].

IC50 & Target

PDEIII[1]
体外研究
(In Vitro)

Anagrelide potently inhibits the development of marrow megakaryocytes (IC50=26 nM)[1].
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[2].
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[3]. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[2]

Cell Line: Megakaryocytic and non-megakaryocytic cells
Concentration: 0.05, 0.3, 1 µM
Incubation Time: 12-day
Result: Inhibited only megakaryocytic cell growth at every concentration tested

体内研究
(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[3]. 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[3]. Anagrelide (5 mg/kg/bid) inhibits or reduces tumor growth in GIST2B, GIST9, GIST882 model models[3].

Shanghai Jinpan Biotech Co Ltd 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/bid
Administration: Treated with 5 mg/kg/bid or with the combination of Anagrelide and Imatinib (given at the same dose and schedule as the single agents); for 10 days
Result: Inhibited or reduced tumor growth in three (GIST2B, GIST9, GIST882) of these four models. The most potent effect was observed in the GIST2B model that harbors a KIT exon 9 mutation leading to p.A502_Y503 duplication. Reduced the tumor volume 68% after 10 days of therapy in this model.

分子量

256.09

Formula

C10H7Cl2N3O
CAS 号

68475-42-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Guosu Wang, et al. Comparison of the biological activities of Anagrelide and its major metabolites in haematopoietic cell cultures. Br J Pharmacol. 2005 Oct;146(3):324-32.

    [2]. Y Hong, et al. Comparison between Anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: selectivity of Anagrelide for the megakaryocytic lineage. Leukemia. 2006 Jun;20(6):1117-22.

    [3]. Olli-Pekka Pulkka, et al. Anagrelide for Gastrointestinal Stromal Tumor. Clin Cancer Res. 2019 Mar 1;25(5):1676-1687.

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