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

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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Other Forms of Anagrelide:

Anagrelide 相关抗体

Top Publications Citing Use of Products

查看 Phosphodiesterase (PDE) 亚型特异性产品:

查看所有亚型
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

  • 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]
细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HeLa EC50
5.12 nM
Compound: 1
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability measured after 72 hrs by MTT assay
[PMID: 37077378]
HeLa EC50
6.67 nM
Compound: 1
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay
[PMID: 37077378]
Platelet EC50
< 1 μg/mL
Compound: 1
Antiplatelet aggregation activity in rabbit platelet-rich plasma assessed as reduction in ADP-induced aggregation incubated for 5 mins by aggregometry
Antiplatelet aggregation activity in rabbit platelet-rich plasma assessed as reduction in ADP-induced aggregation incubated for 5 mins by aggregometry
[PMID: 37077378]
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.

Anagrelide 相关抗体:

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

Anagrelide 相关分类

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  • 稀释计算器

The molarity calculator equation

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

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The dilution calculator equation

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

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× = ×
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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.

Keywords:

Anagrelide68475-42-3Phosphodiesterase (PDE)Apoptosismegakaryocytehaematopoiesisphosphodiesterasemyeloproliferative disordersPhosphodiesteraseplatelet productionimidazoquinazolineantithrombopoieticInhibitorinhibitorinhibit

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