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

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.

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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 Related Antibodies

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Description

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

 

In Vitro

Anagrelide hydrochloride monohydrate potently inhibits the development of marrow megakaryocytes (IC50=26 nM)[1].
Anagrelide (0.05, 0.3, 1 µM; 12-day) hydrochloride monohydrate inhibits only megakaryocytic cell growth not non-megakaryocytic cells[2].
Anagrelide (0.1-10000 nM) hydrochloride monohydrate 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 hydrochloride monohydrate Related Antibodies

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.
In Vivo

Anagrelide (5 mg/kg/bid; for 10 days) hydrochloride monohydrate 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

310.56

Formula

C10H10Cl3N3O2
CAS No.
SMILES

ClC1=C(CN(C2)C3=NC2=O)C(N3)=CC=C1Cl.O.Cl
Shipping

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 hydrochloride monohydrate 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:

Anagrelide hydrochloride823178-43-4Phosphodiesterase (PDE)ApoptosisPhosphodiesterasePDE3imidazoquinazolineplatelet aggregationbone marrow megakaryocytopoiesisgastrointestinal stromal tumorGISTantithrombopoieticInhibitorinhibitorinhibit

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