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VX-702

Name: VX-702
Brand: Selleck Chemicals
SKU: S6005
Rating: 5 (41 reviews)

Catalog No.S6005 Purity:99.94%

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

VX-702 Chemical Structure

CAS No. 745833-23-2

Purity & Quality Control

Batch: Purity: 99.94%

99.94

VX-702 Related Products

Related Targets	p38α p38β	Click to Expand
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Signaling Pathway

p38 MAPK Signaling Pathway

Cell Data

Cell Lines	Assay Type	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 C_max 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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT00395577	Completed	Rheumatoid Arthritis	Vertex Pharmaceuticals Incorporated	November 2006	Phase 2

References

[4] Bhattacharya K, et al. Circulation, 2003, 108(17), 882.

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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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (9.89mM)	Taking the 1 mL working solution as an example, add 50 μL of 80 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

Preparing Stock Solutions

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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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