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

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.

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Anagrelide

Anagrelide 構造式

CAS 番号 : 68475-42-3

容量 価格（税別） 在庫状況 数量
5 mg $62 在庫あり
10 mg $100 在庫あり
25 mg $200 在庫あり
50 mg $300 在庫あり
100 mg $450 在庫あり
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Based on 3 publication(s) in Google Scholar

Other Forms of Anagrelide:

Anagrelide 関連抗体

Top Publications Citing Use of Products

Phosphodiesterase (PDE) アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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  • 参考文献

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製品説明

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]
Cellular Effect
Cell Line Type Value Description References
HeLa EC50
4 nM
Compound: 1
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth
Antiproliferative activity against human HeLa cells assessed as reduction in cell growth
[PMID: 37077378]
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
0.08 μM
Compound: 1
Antiplatelet aggregation activity in human rich plasma assessed as reduction in collagen-induced platelet aggregation
Antiplatelet aggregation activity in human rich plasma assessed as reduction in collagen-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.08 μM
Compound: 1
Antiplatelet aggregation activity in rhesus monkey platelet rich plasma assessed as reduction in collagen-induced platelet aggregation
Antiplatelet aggregation activity in rhesus monkey platelet rich plasma assessed as reduction in collagen-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.15 μM
Compound: 1
Antiplatelet aggregation activity in Sprague-Dawley rat platelet rich plasma assessed as reduction in collagen-induced platelet aggregation
Antiplatelet aggregation activity in Sprague-Dawley rat platelet rich plasma assessed as reduction in collagen-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.27 μM
Compound: 1
Antiplatelet aggregation activity in Sprague-Dawley rat platelet rich plasma assessed as reduction in ADP-induced platelet aggregation
Antiplatelet aggregation activity in Sprague-Dawley rat platelet rich plasma assessed as reduction in ADP-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.31 μM
Compound: 1
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of collagen-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.31 μM
Compound: 1
Antiplatelet aggregation activity in dog rich plasma assessed as reduction in ADP-induced platelet aggregation
Antiplatelet aggregation activity in dog rich plasma assessed as reduction in ADP-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.39 μM
Compound: 1
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of arachidonic acid-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.4 μM
Compound: 1
Antiplatelet aggregation activity in human rich plasma assessed as reduction in ADP-induced platelet aggregation
Antiplatelet aggregation activity in human rich plasma assessed as reduction in ADP-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.5 μM
Compound: 1
Antiplatelet aggregation activity in rhesus monkey platelet rich plasma assessed as reduction in ADP-induced platelet aggregation
Antiplatelet aggregation activity in rhesus monkey platelet rich plasma assessed as reduction in ADP-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.7 μM
Compound: 1
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of thrombin-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
0.74 μM
Compound: 1
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of antigen-antibody-induced platelet aggregation
Antiplatelet activity in rabbit platelet rich plasma assessed as inhibition of antigen-antibody-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
1.2 μM
Compound: 1
Antiplatelet aggregation activity in rabbit platelet rich plasma assessed as reduction in ADP-induced platelet aggregation
Antiplatelet aggregation activity in rabbit platelet rich plasma assessed as reduction in ADP-induced platelet aggregation
[PMID: 37077378]
Platelet EC50
27 nM
Compound: 1
Antiplatelet activity against ADP-induced Wistar rat platelet aggregation assessed as inhibition of platelet aggregation
Antiplatelet activity against ADP-induced Wistar rat platelet aggregation assessed as inhibition of platelet aggregation
[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]
体外実験

Anagrelide potently inhibits the development of marrow megakaryocytes (IC50=26 nM)[1].
Anagrelide (0.05, 0.3, 1 µM; 12-day) inhibits only megakaryocytic cell growth not non-megakaryocytic cells[2].
Anagrelide (0.1-10000 nM) induces a cytotoxic effect in the GIST882 cell line[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Anagrelide 関連抗体

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.
体内実験

Anagrelide (5 mg/kg/bid; for 10 days) inhibits or reduces tumor growth in GIST2B, GIST9, GIST882 model models[3].

MedChemExpress (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.
臨床実験
分子量

256.09

分子式

C10H7Cl2N3O
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=NC3=C(C(Cl)=C(Cl)C=C3)CN2C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 2.56 mg/mL (10.00 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9049 mL 19.5244 mL 39.0488 mL
5 mM 0.7810 mL 3.9049 mL 7.8098 mL
10 mM 0.3905 mL 1.9524 mL 3.9049 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

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体積 （開始）

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Calculation results:
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純度とドキュメンテーション
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9049 mL 19.5244 mL 39.0488 mL 97.6219 mL
5 mM 0.7810 mL 3.9049 mL 7.8098 mL 19.5244 mL
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Anagrelide Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
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.

Keywords:

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

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製品名:
Anagrelide
製品番号:
HY-B0523
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