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| 50mg |
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| 100mg |
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Purity: ≥98%
Anagrelide HCl (formerly BL4162A; BL-4162A; BL-4162-A; trade names Agrylin/Xagrid, Shire and Thromboreductin), the hydrochloride salt of Anagrelide, is an approved drug used for the treatment of essential thrombocytosis (thrombocythemia) and overproduction of blood platelets. It has been reported that Anagrelide acts by inhibiting PDE-3 and phospholipase A but the exact mechanism of action remains unclear.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation No information is available on the use of anagrelide during breastfeeding. The manufacturer recommends that the drug not be used during breastfeeding and for 1 week after the last dose. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
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| References |
Semin Thromb Hemost.1997;23(4):379-83;N Engl J Med.1988 May 19;318(20):1292-4.
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| Additional Infomation |
Anagrelide hydrochloride is the hydrochloride salt of anagrelide. It has a role as an antifibrinolytic drug and a platelet aggregation inhibitor. It contains an anagrelide.
Anagrelide Hydrochloride Anhydrous is the hydrochloride salt of a synthetic quinazoline derivative, Anagrelide Hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. (NCI04) Anagrelide Hydrochloride is the hydrochloride salt of a synthetic quinazoline derivative, Anagrelide Hydrochloride reduces platelet production through a decrease in megakaryocyte maturation. Anagrelide inhibits cyclic AMP phosphodiesterase, as well as ADP- and collagen-induced platelet aggregation. At therapeutic doses, it does not influence white cell counts or coagulation parameters. Anagrelide is used for treatment of essential thrombocythemia to reduce elevated platelet counts and the risk of thrombosis. (NCI04) See also: Anagrelide (annotation moved to). Drug Indication Xagrid is indicated for the reduction of elevated platelet counts in at-risk essential-thrombocythaemia (ET) patients who are intolerant to their current therapy or whose elevated platelet counts are not reduced to an acceptable level by their current therapy. An at-risk patientAn at-risk ET is defined by one or more of the following features: > 60 years of age or; a platelet count > 1000 x 109/l or; a history of thrombohaemorrhagic events. |
| Molecular Formula |
C10H7CL2N3O.HCL
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| Molecular Weight |
292.55
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| Exact Mass |
290.973
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| CAS # |
58579-51-4
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| Related CAS # |
Anagrelide;68475-42-3;Anagrelide hydrochloride monohydrate;823178-43-4
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| PubChem CID |
135413494
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| Appearance |
White to off-white solid powder
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| Density |
1.77g/cm3
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| Boiling Point |
376.5ºC at 760 mmHg
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| Melting Point |
>280ºC
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| Flash Point |
181.5ºC
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| LogP |
2.43
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
17
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| Complexity |
360
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
TVWRQCIPWUCNMI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H7Cl2N3O.ClH/c11-6-1-2-7-5(9(6)12)3-15-4-8(16)14-10(15)13-7;/h1-2H,3-4H2,(H,13,14,16);1H
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| Chemical Name |
Imidazo(2,1-b)quinazolin-2(3H)-one, 6,7-dichloro-1,5-dihydro-, monohydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.77 mg/mL (2.63 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.77 mg/mL (2.63 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 7.7 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.77 mg/mL (2.63 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4182 mL | 17.0911 mL | 34.1822 mL | |
| 5 mM | 0.6836 mL | 3.4182 mL | 6.8364 mL | |
| 10 mM | 0.3418 mL | 1.7091 mL | 3.4182 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02076815 | Completed | Drug: Anagrelide retard Drug: Thromboreductin |
Essential Thrombocythemia | AOP Orphan Pharmaceuticals AG | February 2014 | Phase 3 |
| NCT02125318 | Completed | Drug: Anagrelide CR | Thrombocytosis Myeloproliferative Neoplasms |
Galena Biopharma, Inc. | May 2014 | Phase 2 |
| NCT01552928 | Completed Has Results | Drug: Anagrelide 0.5 mg Drug: Anagrelide 2.5 mg |
Healthy | Shire | March 29, 2012 | Phase 1 |
| NCT01352585 | Completed Has Results | Drug: Anagrelide hydrochloride | Essential Thrombocythemia (ET) | Shire | July 19, 2011 |
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