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 Chemical Structure

Anagrelide Chemical Structure

CAS No. : 68475-42-3

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Based on 2 publication(s) in Google Scholar

Other Forms of Anagrelide:

Anagrelide Related Antibodies

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PDE1 PDE2 PDE3 PDE4 PDE5 PDE6 PDE7 PDE9 PDE10 PDE11 PDE12 PDE8 Autotaxin

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Description

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
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]
In Vitro

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 Related Antibodies

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.
In Vivo

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.
Clinical Trial
Molecular Weight

256.09

Formula

C10H7Cl2N3O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1NC2=NC3=C(C(Cl)=C(Cl)C=C3)CN2C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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
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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

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

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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