1. Metabolic Enzyme/Protease Apoptosis
  2. Phosphodiesterase (PDE) Apoptosis
  3. Anagrelide

Anagrelide  (Synonyms: 阿那格雷)

目录号: HY-B0523
产品使用指南

Anagrelide 是一种有效的 III 型磷酸二酯酶 (PDE3) 抑制剂 (IC50=36 nM)。Anagrelide 是一种咪唑并喹唑啉衍生物,可作为血小板聚集抑制剂。Anagrelide 可抑制骨髓巨核细胞生成。Anagrelide 在体外可降低胃肠道间质瘤 (GIST) 细胞增殖并促进其凋亡。Anagrelide 是一种血小板降低剂,具有抗血栓形成作用。

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Anagrelide Chemical Structure

Anagrelide Chemical Structure

CAS No. : 68475-42-3

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Anagrelide 的其他形式现货产品:

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Anagrelide is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide inhibits bone marrow megakaryocytopoiesis. Anagrelide decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide is a platelet-lowering agent and plays in the antithrombopoietic action[1][2][3].

IC50 & Target

PDEIII[1]

体外研究
(In Vitro)

Anagrelide 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) 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) 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.

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

Cell Cytotoxicity Assay[3]

Cell Line: GIST882 and GIST48 cell line
Concentration: 0.1, 1, 10, 100, 1000, 10000 nM
Incubation Time:
Result: Induced a cytotoxic effect in the GIST882 cell line (IC50= 16 nM), but was only weakly active in the GIST48 cell line.
体内研究
(In Vivo)

Anagrelide (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
分子量

256.09

Formula

C10H7Cl2N3O

CAS 号
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.

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Anagrelide
目录号:
HY-B0523
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