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

Anagrelide hydrochloride monohydrate  (Synonyms: 阿那格雷盐酸盐一水合物)

目录号: HY-B0523B
产品使用指南

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

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Anagrelide hydrochloride monohydrate Chemical Structure

Anagrelide hydrochloride monohydrate Chemical Structure

CAS No. : 823178-43-4

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Anagrelide hydrochloride monohydrate 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 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[1][2][3].

IC50 & Target[2]

PDE3

 

体外研究
(In Vitro)

Anagrelide hydrochloride monohydrate 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 monohydrate 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 monohydrate 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 Viability 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[3]
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) hydrochloride monohydrate 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

310.56

Formula

C10H10Cl3N3O2

CAS 号
中文名称

阿那格雷盐酸盐一水合物

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

Anagrelide hydrochloride monohydrate 相关分类

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The molarity calculator equation

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

质量   浓度   体积   分子量 *
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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 hydrochloride monohydrate
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HY-B0523B
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