1. MAPK/ERK Pathway
  2. p38 MAPK

VX-702 (Synonyms: VX702; VX 702)

Cat. No.: HY-10401 Purity: 99.54%
Data Sheet SDS Handling Instructions

VX-702 is a highly selective inhibitor of p38α MAPK(IC50=4 -20 nM), 14-fold higher potency against the p38α versus p38β.

For research use only. We do not sell to patients.
VX-702 Chemical Structure

VX-702 Chemical Structure

CAS No. : 745833-23-2

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10 mM * 1 mL in DMSO $55 In-stock
10 mg $50 In-stock
50 mg $150 In-stock
100 mg $270 In-stock
200 mg $490 In-stock
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Description

VX-702 is a highly selective inhibitor of p38α MAPK(IC50=4 -20 nM), 14-fold higher potency against the p38α versus p38β. IC50 value: 4-20 nM [1] Target: p38α MAPK 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].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT00395577 Vertex Pharmaceuticals Incorporated Rheumatoid Arthritis November 2006 Phase 2
NCT00205478 Vertex Pharmaceuticals Incorporated Rheumatoid Arthritis June 2005 Phase 2
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References
M.Wt

404.32

Formula

C₁₉H₁₂F₄N₄O₂

CAS No.

745833-23-2

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

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 42 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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VX-702
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