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In Vivo Toxicity and Antithrombotic Profile of the Oral Formulation of the Antileukemic Agent, LFM-A13-F

In Vivo Toxicity and Antithrombotic Profile of the Oral Formulation of the Antileukemic Agent, LFM-A13-F

Heather E Tibbles, Peter Samuel, Doug Erbeck, Sandeep Mahajan, Fatih M Uckun

Arzneimittelforschung. 2004;54(6):330-9.

PMID: 15281619

Abstract:

The specific inhibitor of the protein tyrosine kinase, Bruton's tyrosine kinase (BTK), alpha-cyano-beta-hydroxy-beta-methyl-N-(2,5-dibromophenyl)-propenamide (LFM-A13, CAS 244240-24-2), is a chemosensitizing antileukemic agent with antithrombotic properties. Oral formulation of LFM-A13 (LFM-A13-F) did not cause acute, subacute or chronic toxicity in mice at dose levels up to 200 mg/kg. The in vivo antithrombotic activity of LFM-A13 was studied in a mouse model of collagen-induced fatal thromboembolism. Oral doses of LFM-A13-F dose dependently prevented collagen-induced thromboembolism in mice without causing bleeding. LFM-A13 could be combined with dipyridamole (CAS 58-32-2) without side effects. These results indicate that LFM-A13 may be particularly useful in the treatment of leukemia patients who are at risk for thromboembolic complications.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP62004357	LFM-A13 - CAS 62004-35-7		62004-35-7	Price

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