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VX-702

Name: VX-702
Brand: TargetMol
SKU: T2513
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T2513Cas No. 745833-23-2

Alias 479543-46-9

VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).

VX-702

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Purity: 99.19%

Catalog No. T2513Alias 479543-46-9Cas No. 745833-23-2

Pack Size	Price	USA Warehouse	Global Warehouse
5 mg	$30	In Stock	In Stock
10 mg	$45	In Stock	In Stock
25 mg	$77	In Stock	In Stock
50 mg	$118	In Stock	In Stock
100 mg	$172	-	In Stock
1 mL x 10 mM (in DMSO)	$50	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products. If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.

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Purity:99.19%

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	VX-702 is a highly specific p38α MAPK inhibitor, 14-fold higher selectivity for the p38α than p38β. VX-702 is a small molecule investigational oral anti-cytokine therapy for treatment of inflammatory diseases, specifically rheumatoid arthritis (RA).
Targets&IC50	p38α:4 nM-20 nM
In vitro	Administering VX-702 (0.1 mg/kg) twice daily exhibited effects similar to those of methotrexate (0.1 mg/kg). Furthermore, the efficacy of administering VX-702 (5 mg/kg) twice daily was akin to that of a once-daily dose of prednisolone (10 mg/kg). The MI/AAR ratio in the group treated with VX-702 (50 mg/kg) was significantly lower compared to both the control group and the group treated with VX-702 at 5 mg/kg. VX-702 has a half-life of 16-20 hours, a clearance volume of 3.75 L, and a distribution volume of 73 L/kg. It selectively inhibits the activity of p38 MAPK without affecting ERKs and JNKs.
In vivo	VX-702 does not inhibit platelet aggregation induced by p38 MAPK activators. Treatment with VX-702 (1 μM) can completely or partially suppress p38 activity induced by various platelet activators, including thrombin, AYPGKF, SFLLRN, U46619, and collagen, with an IC50 ranging from 4-20 nM. Additionally, VX-702 dose-dependently inhibits the production of IL-6 (IC50: 59 ng/ml), IL-1β (IC50: 122 ng/ml), and TNFα (IC50: 99 ng/ml).
Kinase Assay	HDAC enzyme assay in vitro: The deacetylase enzyme assay is based on a homogeneous fluorescence release assay. Purified recombinant HDAC enzymes are incubated with MGCD0103 diluted in various concentrations for 10 minutes in assay buffer [25 mM HEPES (pH 8.0), 137 mM NaCl, 1 mM MgCl2, 2.7 mM KCl] at room temperature. The substrate Boc-Lys(ε-Ac)-AMC is added to the reaction for further incubation at 37 °C. The concentration of the substrate and the incubation time varies for different isotypes of HDAC enzymes. A 20-min trypsin incubation at room temperature allows the release of the fluorophore from the deacetylated substrate. The fluorescent signal is detected by fluorometer at excitation of 360 nm, emission of 470 nm, and cutoff at 435 nm.
Synonyms	479543-46-9

Chemical Properties

Molecular Weight	404.32
Formula	C₁₉H₁₂F₄N₄O₂
Cas No.	745833-23-2
Smiles	NC(=O)N(c1ccc(C(N)=O)c(n1)-c1ccc(F)cc1F)c1c(F)cccc1F
Relative Density.	1.503

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 60 mg/mL (148.4 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.95 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.4733 mL	12.3664 mL	24.7329 mL	123.6644 mL
5 mM	0.4947 mL	2.4733 mL	4.9466 mL	24.7329 mL
10 mM	0.2473 mL	1.2366 mL	2.4733 mL	12.3664 mL
20 mM	0.1237 mL	0.6183 mL	1.2366 mL	6.1832 mL
50 mM	0.0495 mL	0.2473 mL	0.4947 mL	2.4733 mL
100 mM	0.0247 mL	0.1237 mL	0.2473 mL	1.2366 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 stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

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

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