1. MAPK/ERK Pathway
    Autophagy
  2. p38 MAPK
    Autophagy
  3. VX-702

VX-702 

Cat. No.: HY-10401 Purity: 99.75%
Handling Instructions

VX-702 is a highly selective inhibitor of p38α MAPK, 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

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 180 In-stock
Estimated Time of Arrival: December 31
100 mg USD 324 In-stock
Estimated Time of Arrival: December 31
200 mg USD 588 In-stock
Estimated Time of Arrival: December 31
500 mg   Get quote  
1 g   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

p38α MAPK[1]

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
Molecular Weight

404.32

Formula

C₁₉H₁₂F₄N₄O₂

CAS No.

745833-23-2

SMILES

O=C(N)C1=CC=C(N=C1C2=CC=C(C=C2F)F)N(C3=C(C=CC=C3F)F)C(N)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 42 mg/mL (103.88 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4733 mL 12.3664 mL 24.7329 mL
5 mM 0.4947 mL 2.4733 mL 4.9466 mL
10 mM 0.2473 mL 1.2366 mL 2.4733 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

VX-702VX702VX 702p38 MAPKAutophagyInhibitorinhibitorinhibit

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VX-702
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HY-10401
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