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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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]
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.
SMILES

O=C1NC2=NC3=C(C(Cl)=C(Cl)C=C3)CN2C1
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Anagrelide Related Classifications

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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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