Anagrelide hydrochloride
Based on 3 publication(s) in Google Scholar
Anagrelide hydrochloride (BL4162A) is a potent inhibitor of phosphodiesterase type III (PDE3) (IC50=36 nM). Anagrelide hydrochloride, an imidazoquinazoline derivative, acts as an inhibitor of platelet aggregation. Anagrelide hydrochloride inhibits bone marrow megakaryocytopoiesis. Anagrelide hydrochloride decreases gastrointestinal stromal tumor (GIST) cell proliferation and promotes their apoptosis in vitro. Anagrelide hydrochloride is a platelet-lowering agent and plays in the antithrombopoietic action.
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- Purity: 99.28%
- CAS No.: 58579-51-4
- 화학식: C10H8Cl3N3O
- 분자량:292.55
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Anagrelide hydrochloride
More
Biological Activity
Anagrelide hydrochloride (BL4162A) potently inhibits the development of marrow megakaryocytes (IC50=26 nM)[1].
Anagrelide (0.05, 0.3, 1 µM; 12-day) hydrochloride inhibits only megakaryocytic cell growth not non-megakaryocytic cells[2].
Anagrelide (0.1-10000 nM) hydrochloride 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.
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Cell Line:Megakaryocytic and non-megakaryocytic cells
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Concentration:0.05, 0.3, 1 µM
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Incubation Time:12-day
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Result:Inhibited only megakaryocytic cell growth at every concentration tested.
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Cell Line:GIST882 and GIST48 cell line
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Concentration:0.1, 1, 10, 100, 1000, 10000 nM
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Incubation Time:
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Result:Induced a cytotoxic effect in the GIST882 cell line (IC50= 16 nM), but was only weakly active in the GIST48 cell line.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Adult female athymic mice bearing GIST2B, GIST3, GIST9, GIST882 model[3]
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Dosage:5 mg/kg
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Administration:Twice daily; for 10 days
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Result:Inhibited or reduced tumor growth in three (GIST2B, GIST9, GIST882) of these four models.
Chemical Information
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CAS No. 58579-51-4
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Appearance Solid
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분자량 292.55
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화학식 C10H8Cl3N3O
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Color White to off-white
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SMILES
ClC1=C(CN(C2)C3=NC2=O)C(N3)=CC=C1Cl.Cl
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Synonyms
BL4162A
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (3)
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Journal Impact Factor
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Most Recent
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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
용액&용해도
DMSO : 6.36 mg/mL (21.74 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)
H2O : < 0.1 mg/mL (insoluble)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 0.77 mg/mL (2.63 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.77 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 0.77 mg/mL (2.63 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 0.77 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (7.7 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Handling Instructions (2659 KB)
References
[1]. Pescatore, S.L. and C. Lindley, Anagrelide: a novel agent for the treatment of myeloproliferative disorders. Expert Opin Pharmacother, 2000. 1(3): p. 537-46. [Content Brief]
[2]. Petrides, P.E., Anagrelide: what was new in 2004 and 2005? Semin Thromb Hemost, 2006. 32(4 Pt 2): p. 399-408. [Content Brief]
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 (sealed storage, away from moisture). 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 | 3.4182 mL | 17.0911 mL | 34.1822 mL | 85.4555 mL |
| 5 mM | 0.6836 mL | 3.4182 mL | 6.8364 mL | 17.0911 mL | |
| 10 mM | 0.3418 mL | 1.7091 mL | 3.4182 mL | 8.5455 mL | |
| 15 mM | 0.2279 mL | 1.1394 mL | 2.2788 mL | 5.6970 mL | |
| 20 mM | 0.1709 mL | 0.8546 mL | 1.7091 mL | 4.2728 mL |
Anagrelide hydrochloride Related Classifications
HY-B0523A Related Classifications
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