Cat. No.: HY-B0523

Anagrelide

3 Cited Publications

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Based on 3 publication(s) in Google Scholar

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.

Purity: 99.87%
CAS No.: 68475-42-3
Formula: C₁₀H₇Cl₂N₃O
Molecular Weight:256.09

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Anagrelide Chemical Structure

CAS No.: 68475-42-3

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
Purity & Documentation
References
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

PDEIII^[1]

All Phosphodiesterase (PDE) Isoforms :

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	<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]
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]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 68475-42-3
Appearance Solid
Molecular Weight 256.09
Formula C₁₀H₇Cl₂N₃O
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

Publications (3)

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Journal Impact Factor

Cell Metab

Imatinib and methazolamide ameliorate COVID-19-induced metabolic complications via elevating ACE2 enzymatic activity and inhibiting viral entry. [Abstract]

2022 Mar 1;34(3):424-440.e7. PMID: 35150639
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Exp Hematol

Purging myeloma cell contaminants and simultaneous expansion of peripheral blood mobilised stem cells. [Abstract]

2024 Mar:131:104138. PMID: 38151170

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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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Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
DMSO	5 mM	0.7810 mL	3.9049 mL	7.8098 mL	19.5244 mL

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Anagrelide

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Publications Citing Use of MedChemExpress (MCE) Anagrelide

All Phosphodiesterase (PDE) Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Anagrelide Related Classifications

HY-B0523 Related Classifications