Home MAPK p38 MAPK inhibitor VX-702 For research use only.

VX-702

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

VX-702 Chemical Structure

VX-702 Chemical Structure

CAS No. 745833-23-2

Purity & Quality Control

VX-702 Related Products

Signaling Pathway

p38 MAPK Signaling Pathways

p38 MAPK Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HOP-62 cell Growth inhibition assay Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.01543 μM SANGER
human NCI-H720 cell Growth inhibition assay Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=0.01682 μM SANGER
JVM-2 cell Growth inhibition assay Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=0.083 μM SANGER
human NCI-H69 cell Growth inhibition assay Inhibition of human NCI-H69 cell growth in a cell viability assay, IC50=0.09941 μM SANGER
human BV-173 cell Growth inhibition assay Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.11386 μM SANGER
human KU812 cell Growth inhibition assay Inhibition of human KU812 cell growth in a cell viability assay, IC50=0.12488 μM SANGER
human DU-145 cell Growth inhibition assay Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.14554 μM SANGER
KARPAS-45 cell Growth inhibition assay Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.14826 μM SANGER
human AGS cell Growth inhibition assay Inhibition of human AGS cell growth in a cell viability assay, IC50=0.15251 μM SANGER
human MOLT-13 cell Growth inhibition assay Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=0.15981 μM SANGER
human NCI-H209 cell Growth inhibition assay Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=0.1758 μM SANGER
human CTV-1 cell Growth inhibition assay Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.18389 μM SANGER
LU-139 cell Growth inhibition assay Inhibition of human LU-139 cell growth in a cell viability assay, IC50=0.19435 μM SANGER
ML-2 cell Growth inhibition assay Inhibition of human ML-2 cell growth in a cell viability assay, IC50=0.22661 μM SANGER
human K5 cell Growth inhibition assay Inhibition of human K5 cell growth in a cell viability assay, IC50=0.22917 μM SANGER
human SBC-1 cell Growth inhibition assay Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=0.2362 μM SANGER
human COR-L88 cell Growth inhibition assay Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=0.3348 μM SANGER
human KY821 cell Growth inhibition assay Inhibition of human KY821 cell growth in a cell viability assay, IC50=0.39603 μM SANGER
human HCC2218 cell Growth inhibition assay Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=0.49728 μM SANGER
human ECC10 cell Growth inhibition assay Inhibition of human ECC10 cell growth in a cell viability assay, IC50=0.65389 μM SANGER
human EW-3 cell Growth inhibition assay Inhibition of human EW-3 cell growth in a cell viability assay, IC50=0.66611 μM SANGER
human EW-18 cell Growth inhibition assay Inhibition of human EW-18 cell growth in a cell viability assay, IC50=0.74679 μM SANGER
human UACC-257 cell Growth inhibition assay Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=1.20326 μM SANGER
human G-361 cell Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=1.49519 μM SANGER
human HMV-II cell Growth inhibition assay Inhibition of human HMV-II cell growth in a cell viability assay, IC50=1.77184 μM SANGER
human DEL cell Growth inhibition assay Inhibition of human DEL cell growth in a cell viability assay, IC50=2.20704 μM SANGER
human IGROV-1 cell Growth inhibition assay Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=2.43188 μM SANGER
human SK-OV-3 cell Growth inhibition assay Inhibition of human SK-OV-3 cell growth in a cell viability assay, IC50=2.61697 μM SANGER
human LAMA-84 cell Growth inhibition assay Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=2.71284 μM SANGER
human NCI-H510A cell Growth inhibition assay Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=2.92526 μM SANGER
human CP66-MEL cell Growth inhibition assay Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=2.93559 μM SANGER
human HAL-01 cell Growth inhibition assay Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=3.27918 μM SANGER
human RS4-11 cell  Growth inhibition assay Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=3.70573 μM SANGER
human RPMI-8226 cell Growth inhibition assay Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50=3.82376 μM SANGER
human NCI-H82 cell Growth inhibition assay Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50=3.89305 μM SANGER
human NY cells Growth inhibition assay Inhibition of human NY cell growth in a cell viability assay, IC50=4.27637 μM SANGER
human MDA-MB-361 cell Growth inhibition assay Inhibition of human MDA-MB-361 cell growth in a cell viability assay, IC50=4.43158 μM SANGER
human MOLT-4 cell Growth inhibition assay Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=4.99193 μM SANGER
human DU-4475 cell Growth inhibition assay Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=5.05565 μM SANGER
human ESS-1 cell Growth inhibition assay Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=5.29179 μM SANGER
human NCI-H1299 cell Growth inhibition assay Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.53033 μM SANGER
human COLO-684 cell Growth inhibition assay Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=5.58165 μM SANGER
human MV-4-11 cell Growth inhibition assay Inhibition of human MV-4-11 cell growth in a cell viability assay, IC50=5.71199 μM SANGER
human D-542MG cell Growth inhibition assay Inhibition of human D-542MG cell growth in a cell viability assay, IC50=6.39272 μM SANGER
human A4-Fuk cell Growth inhibition assay Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=6.43662 μM SANGER
human HL-60 cell Growth inhibition assay Inhibition of human HL-60 cell growth in a cell viability assay, IC50=7.52212 μM SANGER
human NCI-H526 cell Growth inhibition assay Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=7.59801 μM SANGER
human L-363 cell Growth inhibition assay Inhibition of human L-363 cell growth in a cell viability assay, IC50=7.79252 μM SANGER
human A388 cell Growth inhibition assay Inhibition of human A388 cell growth in a cell viability assay, IC50=7.80384 μM SANGER
human MS-1 Growth inhibition assay Inhibition of human MS-1 cell growth in a cell viability assay, IC50=7.83465 μM SANGER
human JAR cell Growth inhibition assay Inhibition of human JAR cell growth in a cell viability assay, IC50=7.84923 μM SANGER
human TI-73 cell Growth inhibition assay Inhibition of human TI-73 cell growth in a cell viability assay, IC50=8.0622 μM SANGER
human CTB-1 cell Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=8.17825 μM SANGER
human SK-NEP-1 cell Growth inhibition assay Inhibition of human SK-NEP-1 cell growth in a cell viability assay, IC50=11.3038 μM SANGER
human HT-29 cell Growth inhibition assay Inhibition of human HT-29 cell growth in a cell viability assay, IC50=13.9111 μM SANGER
human NCI-H1092 cell Growth inhibition assay Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50=14.318 μM SANGER
human KMOE-2 cell Growth inhibition assay Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=14.6178 μM SANGER
human EM-2 cell Growth inhibition assay Inhibition of human EM-2 cell growth in a cell viability assay, IC50=15.2841 μM SANGER
human RT-112 cell Growth inhibition assay Inhibition of human RT-112 cell growth in a cell viability assay, IC50=15.3984 μM SANGER
human DB cell Growth inhibition assay Inhibition of human DB cell growth in a cell viability assay, IC50=15.8513 μM SANGER
human NCI-H1770 cell Growth inhibition assay Inhibition of human NCI-H1770 cell growth in a cell viability assay SANGER
human CAL-54 cell Growth inhibition assay Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=16.73 μM SANGER
human NB14 cell Growth inhibition assay Inhibition of human NB14 cell growth in a cell viability assay, IC50=17.6395 μM SANGER
human RPMI-7951 cell Growth inhibition assay Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50=19.1783 μM SANGER
human T47D cell Growth inhibition assay Inhibition of human T47D cell growth in a cell viability assay, IC50=21.2243 μM SANGER
human A549 cell Growth inhibition assay Inhibition of human A549 cell growth in a cell viability assay, IC50=21.2811 μM SANGER
human A2780 cell Growth inhibition assay Inhibition of human A2780 cell growth in a cell viability assay, IC50=21.8225 μM SANGER
human SK-MEL-24 cell Growth inhibition assay Inhibition of human SK-MEL-24 cell growth in a cell viability assay, IC50=33.0311 μM SANGER
Click to View More Cell Line Experimental Data

Biological Activity

Description VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β.
Features Highly selective, orally active inhibitor of p38 MAPK.
Targets
p38α [1]
(Cell-free assay)
4 nM-20 nM
In vitro
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
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. In addition, VX-702 (5 mg/kg twice 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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00395577 Completed
Rheumatoid Arthritis
Vertex Pharmaceuticals Incorporated
 November 2006 Phase 2

Chemical Information & Solubility

Molecular Weight 404.3 Formula

C19H12F4N4O2
CAS No. 745833-23-2 SDF Download VX-702 SDF
Smiles C1=CC(=C(C(=C1)F)N(C2=NC(=C(C=C2)C(=O)N)C3=C(C=C(C=C3)F)F)C(=O)N)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 81 mg/mL ( (200.34 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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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.

Handling Instructions

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