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BMS-509744

Catalog No. T14674Cas No. 439575-02-7

BMS-509744 is an inhibitor of ATP competitive Itk (IC50: 19 nM).

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Pack Size	Price	Availability
25 mg	$689	6-8 weeks
50 mg	$896	6-8 weeks
100 mg	$1,350	6-8 weeks

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Product Introduction

Bioactivity

Description	BMS-509744 is an inhibitor of ATP competitive Itk (IC50: 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].

Chemical Properties

Molecular Weight	623.83
Formula	C32H41N5O4S2
Cas No.	439575-02-7

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 21.9 mg/mL (35.11 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.6030 mL	8.0150 mL	16.0300 mL	80.1500 mL
5 mM	0.3206 mL	1.6030 mL	3.2060 mL	16.0300 mL
10 mM	0.1603 mL	0.8015 mL	1.6030 mL	8.0150 mL
20 mM	0.0802 mL	0.4008 mL	0.8015 mL	4.0075 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:

For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . TargetMol | Animal experiments

A total of 10 animals were administered, and the formula you used is 5% TargetMol | reagent

DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

You can also refer to dose conversion for different animals. More

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

BMS-509744BMS 509744BMS509744