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BMS-509744

Chemical Structure : BMS-509744

CAS No.: 439575-02-7

BMS-509744 (BMS 509744, BMS509744)

Catalog No.: PC-42806Not For Human Use, Lab Use Only.

BMS-509744 is a potent, selective, ATP-competitive IL2--inducible T cell kinase (ITK) inhibitor with IC50 of 19 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BMS-509744 is a potent, selective, ATP-competitive IL2--inducible T cell kinase (ITK) inhibitor with IC50 of 19 nM.
BMS-509744 displays >200-fold selectivity over others Tec family tyrosine kinases and > 30-fold over a broad panel protein kinases.
BMS-509744 reduces TCR-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion and T-cell proliferation in vitro.
BMS-509744 significantly diminishes lung inflammation in mouse model of allergy/asthma; also potently blocks wild-type HIV-1 infectivity and replication in vitro.

Physicochemical Properties

M.Wt 623.829
Formula C32H41N5O4S2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: 21.9 mg/mL; in vivo: suspended with formulation of H2O:ethanol:Tween 80=90:5:5.

Chemical Name/SMILES

Benzamide, N-[5-[[5-[(4-acetyl-1-piperazinyl)carbonyl]-4-methoxy-2-methylphenyl]thio]-2-thiazolyl]-4-[[(1,2,2-trimethylpropyl)amino]methyl]-

References

1. Lin TA, et al. Biochemistry. 2004 Aug 31;43(34):11056-62.

2. Dondorf S, et al. J Biol Chem. 2015 Apr 17;290(16):10568-9.

3. Tarafdar S, et al. J Biol Chem. 2014 May 30;289(22):15718-28.

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