VX-702

Catalog No.S6005

VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.

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VX-702 Chemical Structure

VX-702 Chemical Structure
Molecular Weight: 404.3

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Related Compound Libraries

VX-702 is available in the following compound libraries:

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Product Information

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  • Research Area

Product Description

Biological Activity

Description VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β. Phase 2.
Targets p38α [1]
(Cell-free assay)
IC50 4 nM-20 nM
In vitro Pre-incubation of platelets with VX-702 (1 μM) completely or partially inhibits p38 activation (IC50 4 to 20 nM) induced by platelet agonists including thrombin, SFLLRN, AYPGKF, U46619 and collagen. VX-702 shows no effect on platelet aggregation induced by any of the p38 MAPK agonists in the presence or absence of anti-platelet therapies. [1] VX-702 inhibits the production of IL-6, IL-1β and TNFα (IC50 = 59, 122 and 99 ng/mL, respectively) in a dose-dependent manner. [2]
In vivo The half-life of VX-702 is 16 to 20 hours, with a median clearance of 3.75 L/h and a volume of distribution of 73 L/kg. Both AUC and Cmax values are dose proportional for VX-702, which is predominantly cleared renally. [2] VX-702 (at a dose of 0.1 mg/kg twice daily) has an equivalent effect as that of methotrexate (0.1 mg/kg). In addition, VX-702 (5 mg/kg twice daily) also has an equivalent effect as prednisolone (10 mg/kg once daily), as measured by percentage inhibition of wrist joint erosion and inflammation score. [3] VX-702 selectively inhibits activation of p38 MAPK after ischemia with no effects on ERKs and JNKs. The MI/AAR ratio is significantly reduced in the 50 mg/kg group compared with the 5 mg/kg and vehicle groups.[4]
Features Highly selective, orally active inhibitor of p38 MAPK.

Protocol(Only for Reference)

Animal Study: [3]

Animal Models Mouse with collagen-induced arthritis
Formulation
Dosages ≤10 mg/kg
Administration Administered via p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Kuliopulos A, et al. Thromb Haemost, 2004, 92(6), 1387-1393.

[2] Braddock M, IDDB Meeting Report, 2005, March 14-15.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-23)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT00395577 Completed Rheumatoid Arthritis Vertex Pharmaceuticals Incorporated November 2006 Phase 2
NCT00205478 Completed Rheumatoid Arthritis Vertex Pharmaceuticals Incorporated June 2005 Phase 2

Chemical Information

Download VX-702 SDF
Molecular Weight (MW) 404.3
Formula

C19H12F4N4O2

CAS No. 745833-23-2
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 81 mg/mL (200.34 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% PEG400+0.5% Tween80+5% propylene glycol 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name 1-(5-carbamoyl-6-(2,4-difluorophenyl)pyridin-2-yl)-1-(2,6-difluorophenyl)urea

Customer Product Validation(2)


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Rating
Source Mol Immunol 2014 62(2), 266-76. VX-702 purchased from Selleck
Method Cell viability assay
Cell Lines B cells
Concentrations 10 uM
Incubation Time 1 h
Results VX-702 inhibits the α isoform of this MAPK and belongs to the so-called “third generation” of p38 inhibitors that are characterized for acting in a much more selective manner with respect, for example, to SB203580. The levels of IL-10 detected in cell supernatants were decreased when TLR4- or TLR9-stimulated B cells were treated with 10 uM VX-702.

Click to enlarge
Rating
Source Lee lay hoon from National University of Singapore. VX-702 purchased from Selleck
Method ELISA
Cell Lines Bone marrow derived macrophages
Concentrations 1-50 μM
Incubation Time 24 h
Results VX-702 treatment resulted in a reduction of TNF-a production.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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