Anagrelide
featured

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 317191

CAS#: 68475-42-3 (free base)

Description: Anagrelide (Agrylin/Xagrid, Shire and Thromboreductin, AOP Orphan Pharmaceuticals) is a drug used for the treatment of essential thrombocytosis (ET; essential thrombocythemia), or overproduction of blood platelets. It also has been used in the treatment of chronic myeloid leukemia. Anagrelide works by inhibiting the maturation of platelets from megakaryocytes. The mechanism of action of anagrelide is as a Phosphodiesterase 3 Inhibitor. The physiologic effect of anagrelide is by means of Decreased Platelet Production. Anagrelide is a synthetic quinazoline derivative, Anagrelide 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.


Chemical Structure

img
Anagrelide
CAS# 68475-42-3 (free base)

Theoretical Analysis

MedKoo Cat#: 317191
Name: Anagrelide
CAS#: 68475-42-3 (free base)
Chemical Formula: C10H7Cl2N3O
Exact Mass: 254.99662
Molecular Weight: 256.09
Elemental Analysis: C, 46.90; H, 2.76; Cl, 27.69; N, 16.41; O, 6.25

Size Price Shipping out time Quantity
25mg USD 270 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2021-03-01. Prices are subject to change without notice.

Anagrelide purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Related CAS #: 68475-42-3 (free base); 58579-51-4 (hydrochloride)  

Synonym: Agrelin; Agrylin; Anagrelide; Anagrelide; BL 4162A; Xagrid; Shire; Thromboreductin

IUPAC/Chemical Name: 6,7-dichloro-5,10-dihydro-3H-imidazo[2,1-b]quinazolin-2-one

InChi Key: OTBXOEAOVRKTNQ-UHFFFAOYSA-N

InChi Code: InChI=1S/C10H7Cl2N3O/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)

SMILES Code: C1C2=C(C=CC(=C2Cl)Cl)NC3=NC(=O)CN31

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Handling Instructions:

Preparing Stock Solutions

The following data is based on the product molecular weight 256.09 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

1: Antelo ML, de Las Heras N, Gonzalez Porras JR, Kerguelen A, Raya JM. Management of side effects of BCR/ABL-negative chronic myeloproliferative neoplasm therapies. Focus on anagrelide. Expert Rev Hematol. 2015 Dec;8(6):819-35. doi: 10.1586/17474086.2015.1088779. Epub 2015 Sep 14. PubMed PMID: 26368319.

2: Ge X, Yang L, Jin J, Qian W, Li J, Yang R, Cao X, Jiang B, Wang Z, Hou M, Zhang W, Xiao Z, Zhao Y, Gao D, Zhang X, Wang S, Sun A, Fu J, Su L, Li K. [Efficacy and safety of anagrelide in treatment of essential thrombocythemia: multicenter, randomized controlled clinical trial]. Zhonghua Xue Ye Xue Za Zhi. 2015 Jul;36(7):547-52. doi: 10.3760/cma.j.issn.0253-2727.2015.07.00. Chinese. PubMed PMID: 26304075.

3: Mela Osorio MJ, Ferrari L, Goette NP, Gutierrez MI, Glembotsky AC, Maldonado AC, Lev PR, Alvarez C, Korin L, Marta RF, Molinas FC, Heller PG. Long-term follow-up of essential thrombocythemia patients treated with anagrelide: subgroup analysis according to JAK2/CALR/MPL mutational status. Eur J Haematol. 2015 Jun 27. doi: 10.1111/ejh.12614. [Epub ahead of print] PubMed PMID: 26119186.

4: Cascavilla N, De Stefano V, Pane F, Pancrazzi A, Iurlo A, Gobbi M, Palandri F, Specchia G, Liberati AM, D'Adda M, Gaidano G, Fjerza R, Achenbach H, Smith J, Wilde P, Vannucchi AM. Impact of JAK2(V617F) mutation status on treatment response to anagrelide in essential thrombocythemia: an observational, hypothesis-generating study. Drug Des Devel Ther. 2015 May 18;9:2687-94. doi: 10.2147/DDDT.S79576. eCollection 2015. PubMed PMID: 26028965; PubMed Central PMCID: PMC4441358.

5: Samuelson B, Chai-Adisaksopha C, Garcia D. Anagrelide compared with hydroxyurea in essential thrombocythemia: a meta-analysis. J Thromb Thrombolysis. 2015 Nov;40(4):474-9. doi: 10.1007/s11239-015-1218-2. PubMed PMID: 25894476.

6: Kremyanskaya M, Mascarenhas J, Hoffman R. Anagrelide hydrochloride and ruxolitinib for treatment of polycythemia vera. Expert Opin Pharmacother. 2015 Jun;16(8):1185-94. doi: 10.1517/14656566.2015.1036029. Epub 2015 Apr 14. Review. PubMed PMID: 25873215.

7: Ahluwalia M, Butcher L, Donovan H, Killick-Cole C, Jones PM, Erusalimsky JD. The gene expression signature of anagrelide provides an insight into its mechanism of action and uncovers new regulators of megakaryopoiesis. J Thromb Haemost. 2015 Jun;13(6):1103-12. doi: 10.1111/jth.12959. Epub 2015 May 9. PubMed PMID: 25851510.

8: Tortorella G, Piccin A, Tieghi A, Marcheselli L, Steurer M, Gastl G, Codeluppi K, Fama A, Santoro U, Birtolo C, Gugliotta G, Cortelazzo S, Gugliotta L; Gimema Foundation project “Registro Italiano Trombocitemie (RIT)”. Anagrelide treatment and cardiovascular monitoring in essential thrombocythemia. A prospective observational study. Leuk Res. 2015 Jun;39(6):592-8. doi: 10.1016/j.leukres.2015.03.014. Epub 2015 Mar 28. PubMed PMID: 25850727.

9: Schwarz J, Ovesná P, Černá O, Kissová J, Soukupová JM, Brychtová Y, Doubek M, Červinek L, Cmunt E, Dulíček P, Campr V, Křen L, Penka M; for CZEMP - Czech Group for Ph- Myeloproliferative Disorders. Thrombosis in thrombocythemic Ph- myeloproliferations is associated with higher platelet count prior to the event: results of analyses of prothrombotic risk factors from a registry of patients treated with anagrelide. Eur J Haematol. 2015 Mar 25. doi: 10.1111/ejh.12554. [Epub ahead of print] PubMed PMID: 25807961.

10: Espasandin YR, Glembotsky AC, Grodzielski M, Lev PR, Goette NP, Molinas FC, Marta RF, Heller PG. Anagrelide platelet-lowering effect is due to inhibition of both megakaryocyte maturation and proplatelet formation: insight into potential mechanisms. J Thromb Haemost. 2015 Apr;13(4):631-42. doi: 10.1111/jth.12850. Epub 2015 Feb 18. PubMed PMID: 25604267.