[CAS NO. 439575-02-7] BMS-509744
PRODUCTS SPECIFICATIONS [439575-02-7]
DESCRIPTION [439575-02-7]
Overview
| MDL | MFCD18782598 |
|---|---|
| Molecular Weight | 623.83 |
| Molecular Formula | C32H41N5O4S2 |
| SMILES | CC(C(C)(C)C)NCC1=CC=C(C(NC2=NC=C(SC3=CC(C(N4CCN(C(C)=O)CC4)=O)=C(OC)C=C3C)S2)=O)C=C1 |
4 Publications Citing Use of MCE
Summary
BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC 50 of 19 nM.
IC50 & Target
IC50: 19 nM (Itk) [1]
In Vitro
BMS-509744 reduces T-cell receptor-induced functions including PLCγ1 tyrosine phosphorylation, calcium mobilization, IL-2 secretion, and T-cell proliferation in vitro in both human and mouse cells. BMS-488516 and BMS-509744 potently inhibit Itk in vitro with IC 50 values of 96 and 19 nM, respectively. Both compounds exhibit competitive kinetics with respect to ATP, suggesting that they bind to the ATP binding site of the Itk kinase domain [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
BMS-509744 and BMS-488516 suppress the production of IL-2 induced by anti-T-cell receptor antibody administered to mice. BMS-509744 exhibits a 50% inhibitory capacity when dosed at 50 mg/kg, irrespective of the amount of induction antibody. BMS-509744 also significantly diminishes lung inflammation in a mouse model of ovalbumin-induced allergy/asthma [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 21.9 mg/mL ( 35.11 mM ; Need ultrasonic and warming)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.6030 mL | 8.0150 mL | 16.0300 mL |
| 5 mM | 0.3206 mL | 1.6030 mL | 3.2060 mL |
| 10 mM | 0.1603 mL | 0.8015 mL | 1.6030 mL |
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Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution