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Anagrelide hydrochloride

pharmaceutical raw materials
Anagrelide hydrochloride structure

Anagrelide hydrochloride 

structure
  • CAS No:

    58579-51-4

  • Formula:

    C10H7Cl2N3O.ClH

  • Chemical Name:

    Anagrelide hydrochloride

  • Synonyms:

    Imidazo[2,1-b]quinazolin-2(3H)-one,6,7-dichloro-1,5-dihydro-,hydrochloride (1:1);Imidazo[2,1-b]quinazolin-2(3H)-one,6,7-dichloro-1,5-dihydro-,monohydrochloride;BL 4162A;Anagrelide hydrochloride;Agrelin;BMY 26538-01;Agrylin;6,7-Dichloro-1,5-dihydroimidazo[2,1-b]quinazolin-2(3H)-one Hydrochloride

  • Categories:

    Biochemical Engineering  >  Inhibitors

Description

Anagrelide Hydrochloride(BL4162A) is a drug used for the treatment of essential thrombocytosis.Target: PDEAnagrelide hydrochloride is an oral imidazoquinazoline agent that has been shown to reduce elevated platelet counts and the risk of thrombosis in patients with thrombocythaemia in various myeloproliferative disorders (MPD). It is currently approved by the FDA as oral treatment for essential thrombocythaemia (ET) and thrombocythaemia associated with polycythaemia vera (PV). Anagrelide


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 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 Basic Attributes

292.55

290.973297

1308068-626-2

VNS4435G39

759170|724577

DTXSID0046725

C28826

L01XX35

2933990090

Characteristics

44.7

white to beige

1.77g/cm3

>280 °C

181.5ºC

DMSO: soluble 1mg/mL, clear (warmed)

Desiccate at +4°C

6.8X10-10 mm Hg at 25 deg C /Estimated/

147.9 Ų [M+H]+ [CCS Type: TW, Method: calibrated with polyalanine and drug standards]

Safety Information

NONH for all modes of transport

3

22-36/37/38

26

Xn

P261-P305 + P351 + P338

H302-H315-H319-H335

|Danger|H302 (82.35%): Harmful if swallowed [Warning Acute toxicity, oral]|P201, P202, P261, P264, P270, P271, P280, P281, P301+P312, P302+P352, P304+P340, P305+P351+P338, P308+P313, P312, P321, P330, P332+P313, P337+P313, P362, P403+P233, P405, and P501|Aggregated GHS information provided by 51 companies from 5 notifications to the ECHA C&L Inventory. Each notification may be associated with multiple companies.

Drug Information

Anagrelide 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 essential thrombocythaemia patient is defined by one or more of the following features:>60 years of age ora platelet count >1,000 x 10⁹/l ora history of thrombo-haemorrhagic events. 

Fibrinolysin or agents that convert plasminogen to FIBRINOLYSIN. (See all compounds classified as Fibrinolytic Agents.)|Drugs or agents which antagonize or impair any mechanism leading to blood platelet aggregation, whether during the phases of activation and shape change or following the dense-granule release reaction and stimulation of the prostaglandin-thromboxane system. (See all compounds classified as Platelet Aggregation Inhibitors.)

6,7-dichloro-1,5-dihydroimidazo(2,1-b)quinazolin-2(3H)-one hydrochloride

Anagrelide hydrochloride Use and Manufacturing

Methods of Manufacturing

In a 100 ml round-bottom flask anagrelide (0.50 g, 1.952 mmol) was stirred in DMSO (4 ml) to give a white suspension. The mixture was heated on an oil bath. At 50°C, concentrated hydrochloric acid (0.22 ml, 2.48 mmol) was added. An almost clear solution was obtained after further heating. Ethanol (9 ml) was added, and the clear yellow/orange solution was allowed to cool to room temperature. At 40°C (internal temperature), the solution was seeded with anagrelide hydrochloride crystals. A white suspension was obtained. The suspension was filtered over a glass filter, and the crystalline solid was washed with ethanol, and dried on the air, giving anagrelide hydrochloride (255 mg, 0.863 mmol, 44.2 percent yield) as a white crystalline solid.

Uses

Signal Transduction Agents, Potent PDE3 inhibitor

Human drugs -> Anagrelide Mylan -> EMA Drug Category|Antineoplastic agents -> Human pharmacotherapeutic group|Human drugs -> Rare disease (orphan)|Human Drugs -> FDA Approved Drug Products with Therapeutic Equivalence Evaluations (Orange Book) -> Active Ingredients

Computed Properties

Molecular Weight:292.5
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:2
Exact Mass:290.973295
Monoisotopic Mass:290.973295
Topological Polar Surface Area:44.7
Heavy Atom Count:17
Complexity:360
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes

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