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