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BMS-509744 is an inhibitor of ATP competitive Itk (IC50: 19 nM).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
25 mg | $689 | 6-8 weeks | |
50 mg | $896 | 6-8 weeks | |
100 mg | $1,350 | 6-8 weeks |
Description | BMS-509744 is an inhibitor of ATP competitive Itk (IC50: 19 nM). |
Targets&IC50 | ITK:19 nM |
In vitro | BMS-488516 and BMS-509744 effectively inhibit Itk in vitro, demonstrating IC50 values of 96 and 19 nM, respectively. Their competitive kinetics regarding ATP indicate binding to the ATP-binding site of the Itk kinase domain[1]. BMS-509744 also diminishes T-cell receptor-mediated responses, including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in human and mouse cells in vitro. |
In vivo | BMS-509744 demonstrates a 50% inhibitory effect at a dosage of 50 mg/kg, regardless of the induction antibody level. Both BMS-509744 and BMS-488516 inhibit IL-2 production triggered by anti-T-cell receptor antibody in mice. Moreover, BMS-509744 significantly reduces lung inflammation in a mouse model of ovalbumin-induced allergy/asthma[1]. |
Molecular Weight | 623.83 |
Formula | C32H41N5O4S2 |
Cas No. | 439575-02-7 |
Relative Density. | 1.31g/cm3 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||
Solubility Information | DMSO: 21.9 mg/mL (35.11 mM), Sonication and heating are recommended. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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