BMS-509744

Name: BMS-509744
Brand: MedChemExpress
SKU: HY-11092
Rating: 5.0 (5 reviews)

製品番号: HY-11092 純度: 98.05%: Data Sheet SDS COA 取扱説明書
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BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC₅₀ of 19 nM.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 439575-02-7

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 158	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 158	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$115	在庫あり	Estimated Time of Arrival: December 31
10 mg	$200	在庫あり	Estimated Time of Arrival: December 31
25 mg	$450	在庫あり	Estimated Time of Arrival: December 31
50 mg	$800	在庫あり	Estimated Time of Arrival: December 31
100 mg	$1280	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

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* アイテムを追加する前、数量をご選択ください

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Based on 5 publication(s) in Google Scholar

顧客検証

: BMS-509744 purchased from MedChemExpress. Usage Cited in: Cancer Cell Int. 2019 Feb 14:19:32. [Abstract]; Cells are treated with indicated concentrations of BMS-509744 for 24 h, then whole cell lysates are detected by western blot for phosphorylated FAK and total RhoA.

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製品説明

BMS-509744 is a potent, selective and ATP competitive Itk inhibitor with an IC₅₀ of 19 nM.

IC₅₀ & Target

IC50: 19 nM (Itk)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
EL4	IC₅₀	0.07 μM Compound: 3	Inhibition of anti CD3-induced IL2 secretion in mouse EL4 cells Inhibition of anti CD3-induced IL2 secretion in mouse EL4 cells	[PMID: 16682193]
Jurkat	IC₅₀	0.25 μM Compound: 3	Inhibition of anti CD3-induced IL2 secretion in human Jurkat T cells Inhibition of anti CD3-induced IL2 secretion in human Jurkat T cells	[PMID: 16682193]
Jurkat	IC₅₀	250 nM Compound: 3	Inhibition of IL2 production in Jurkat T cells Inhibition of IL2 production in Jurkat T cells	[PMID: 16682193]
PBMC	IC₅₀	0.39 μM Compound: 3	Inhibition of anti CD3-induced IL2 secretion in human PBMC Inhibition of anti CD3-induced IL2 secretion in human PBMC	[PMID: 16682193]
Splenocyte	IC₅₀	0.38 μM Compound: 3	Inhibition of anti CD3-induced IL2 secretion in mouse splenocytes Inhibition of anti CD3-induced IL2 secretion in mouse splenocytes	[PMID: 16682193]
T-cell	IC₅₀	0.43 μM Compound: Chemical probe: BMS-509744	Anti-proliferative activity against irradiated APC induced human T cell incubated for 3 days Anti-proliferative activity against irradiated APC induced human T cell incubated for 3 days	[PMID: 15323564]

体外実験

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 IC₅₀ 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

体内実験

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

623.83

分子式

C₃₂H₄₁N₅O₄S₂

CAS 番号

439575-02-7

Appearance

Solid

Color

White to light yellow

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

DMSO : 66.67 mg/mL (106.87 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.01 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

純度とドキュメンテーション

純度: 98.05%

Select Batch:

データシート (274 KB) SDS (251 KB)

COA (249 KB) LCMS (87 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Lin TA, et al. Selective Itk inhibitors block T-cell activation and murine lung inflammation. Biochemistry.?2004 Aug 31;43(34):11056-62. [Content Brief]

キナーゼ実験 ^[1]	BMS-509744 activity (IC₅₀) is determined by kinase assays. The kinase reactions are performed in the presence of 10 μM GST-SLP-76 and various concentrations of ATP for 10 min using 10 ng of enzyme. The concentrations of BMS-509744 MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[1]	Mice: Balb/c mice are injected subcutaneously with the compounds (BMS-509744 and BMS-488516) or vehicle (H2O:ethanol:Tween 80 ) 90:5:5) 15 min before intravenous administration of anti-CD3 antibody. Serum is collected for the analysis of IL-2 and compound levels at 90 min after anti-CD3 antibody administration. IL-2 is measured by ELISA, and compound levels are measured by mass spectrometry^[1]. MedChemExpress (MCE) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[1]. Lin TA, et al. Selective Itk inhibitors block T-cell activation and murine lung inflammation. Biochemistry.?2004 Aug 31;43(34):11056-62. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	1.6030 mL	8.0150 mL	16.0300 mL	40.0750 mL
	5 mM	0.3206 mL	1.6030 mL	3.2060 mL	8.0150 mL
	10 mM	0.1603 mL	0.8015 mL	1.6030 mL	4.0075 mL
	15 mM	0.1069 mL	0.5343 mL	1.0687 mL	2.6717 mL
	20 mM	0.0802 mL	0.4008 mL	0.8015 mL	2.0038 mL
	25 mM	0.0641 mL	0.3206 mL	0.6412 mL	1.6030 mL
	30 mM	0.0534 mL	0.2672 mL	0.5343 mL	1.3358 mL
	40 mM	0.0401 mL	0.2004 mL	0.4008 mL	1.0019 mL
	50 mM	0.0321 mL	0.1603 mL	0.3206 mL	0.8015 mL
	60 mM	0.0267 mL	0.1336 mL	0.2672 mL	0.6679 mL
	80 mM	0.0200 mL	0.1002 mL	0.2004 mL	0.5009 mL
	100 mM	0.0160 mL	0.0802 mL	0.1603 mL	0.4008 mL

BMS-509744 Related Classifications

Inflammation/Immunology

Molarity Calculator
Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-509744439575-02-7BMS509744BMS 509744ItkInterleukin-2 inducible T-cell kinaseIL2 inducible T-cell kinaseInhibitorinhibitorinhibit

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BMS-509744

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•関連スクリーニングライブラリ:

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純度とドキュメンテーション

参考文献

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BMS-509744 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

BMS-509744 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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