Drug intelligence / Profile preview

BMS-509744

Development stage
Preclinical
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral, Topical
01

Overview

**BMS-509744** is a potent and selective small molecule inhibitor of interleukin-2-inducible T cell kinase (ITK), a member of the Tec family of tyrosine kinases essential for T cell receptor (TCR) signaling. It exhibits high selectivity for ITK (IC50 = 19 nM), with markedly less activity against related kinases, blocking ITK-dependent phosphorylation events and downstream signaling, including PLCγ1 activation, calcium mobilization, IL-2 secretion, and T cell proliferation[1][3][5]. BMS-509744 reduces inflammation and immune cell infiltration in models of allergy, asthma, and autoimmune arthritis, and has shown anti-proliferative and pro-apoptotic effects in T cell lymphoma models both in vitro and in vivo[2][4][6][8]. Developed by Bristol Myers Squibb as a chemical probe, it is widely used in preclinical research and has been investigated for potential immunosuppressive, anti-inflammatory, and anti-tumor activities[9][10].

Other names
Benzamide, N-(5-((5-((4-acetyl-1-piperazinyl)carbonyl)-4-methoxy-2-methylphenyl)thio)-2-thiazolyl)-4-(((1,2,2-trimethylpropyl)amino)methyl)-N-[5-[5-(4-acetylpiperazine-1-carbonyl)-4-methoxy-2-methylphenyl]sulfanyl-1,3-thiazol-2-yl]-4-[(3,3-dimethylbutan-2-ylamino)methyl]benzamideCAS 439575-02-7CAS439575-02-7CAS-439575-02-7
02

Targets

ITK (Interleukin 2-inducible T-cell kinase)

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