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BMS-509744

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Catalog No. T14674Cas No. 439575-02-7

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

BMS-509744

BMS-509744

😃Good
Catalog No. T14674Cas No. 439575-02-7
BMS-509744 is an inhibitor of ATP competitive Itk (IC50: 19 nM).
Pack SizePriceAvailabilityQuantity
25 mg$6896-8 weeks
50 mg$8966-8 weeks
100 mg$1,3506-8 weeks
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight623.83
FormulaC32H41N5O4S2
Cas No.439575-02-7
Relative Density.1.31g/cm3
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM1.6030 mL8.0150 mL16.0300 mL80.1500 mL
5 mM0.3206 mL1.6030 mL3.2060 mL16.0300 mL
10 mM0.1603 mL0.8015 mL1.6030 mL8.0150 mL
20 mM0.0802 mL0.4008 mL0.8015 mL4.0075 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:
TargetMol | Animal experimentsFor 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 DMSOTargetMol | 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 DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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Dose Conversion

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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

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