Anagrelide

Cat. No.: HY-B0523: FAQs
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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.

For research use only. We do not sell to patients.

Anagrelide Chemical Structure

CAS No. : 68475-42-3

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Other In-stock Forms of Anagrelide:

Anagrelide hydrochloride

Other Forms of Anagrelide:

Anagrelide hydrochloride In-stock
Anagrelide-¹³C₂,¹⁵N,d₂ Get quote
Anagrelide hydrochloride monohydrate Get quote

2 Publications Citing Use of MCE Anagrelide

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Biological Activity
Purity & Documentation
References
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Description

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.

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.

68475-42-3

SMILES

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

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

Handling Instructions (2659 KB)

References

[1]. Guosu Wang, et al. Comparison of the biological activities of Anagrelide and its major metabolites in haematopoietic cell cultures. Br J Pharmacol. 2005 Oct;146(3):324-32. [Content Brief]

[2]. Y Hong, et al. Comparison between Anagrelide and hydroxycarbamide in their activities against haematopoietic progenitor cell growth and differentiation: selectivity of Anagrelide for the megakaryocytic lineage. Leukemia. 2006 Jun;20(6):1117-22. [Content Brief]

[3]. Olli-Pekka Pulkka, et al. Anagrelide for Gastrointestinal Stromal Tumor. Clin Cancer Res. 2019 Mar 1;25(5):1676-1687. [Content Brief]

Anagrelide Related Classifications

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The molarity calculator equation

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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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