pour la recherche uniquement

VX-702 p38 MAPK inhibiteur

Name: VX-702
Brand: Selleck Chemicals
SKU: S6005
Rating: 5 (42 reviews)

Réf. CatalogueS6005

Le VX-702 est un inhibiteur hautement sélectif de la p38α MAPK, avec une puissance 14 fois supérieure contre la p38α par rapport à la p38β.

VX-702 p38 MAPK inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 404.3

Aller à

Contrôle Qualité

Lot : Pureté : 99.94%

99.94

Cibles apparentées	ERK Raf JNK MEK Ras KRas S6 Kinase MAP4K TAK1 Mixed Lineage Kinase
Autre p38 MAPK Inhibiteurs	SB202190 SB203580 (Adezmapimod) PH-797804 Doramapimod (BIRB 796) Ralimetinib (LY2228820) dimesylate Losmapimod SB239063 Neflamapimod (VX-745) BMS-582949 Skepinone-L

Culture cellulaire, traitement et concentration de travail

Lignées cellulaires	Type dessai	Description de lactivité
HOP-62 cell	Growth inhibition assay	Inhibition of human HOP-62 cell growth in a cell viability assay, IC50=0.01543 μM
human NCI-H720 cell	Growth inhibition assay	Inhibition of human NCI-H720 cell growth in a cell viability assay, IC50=0.01682 μM
JVM-2 cell	Growth inhibition assay	Inhibition of human JVM-2 cell growth in a cell viability assay, IC50=0.083 μM
human NCI-H69 cell	Growth inhibition assay	Inhibition of human NCI-H69 cell growth in a cell viability assay, IC50=0.09941 μM
human BV-173 cell	Growth inhibition assay	Inhibition of human BV-173 cell growth in a cell viability assay, IC50=0.11386 μM
human KU812 cell	Growth inhibition assay	Inhibition of human KU812 cell growth in a cell viability assay, IC50=0.12488 μM
human DU-145 cell	Growth inhibition assay	Inhibition of human DU-145 cell growth in a cell viability assay, IC50=0.14554 μM
KARPAS-45 cell	Growth inhibition assay	Inhibition of human KARPAS-45 cell growth in a cell viability assay, IC50=0.14826 μM
human AGS cell	Growth inhibition assay	Inhibition of human AGS cell growth in a cell viability assay, IC50=0.15251 μM
human MOLT-13 cell	Growth inhibition assay	Inhibition of human MOLT-13 cell growth in a cell viability assay, IC50=0.15981 μM
human NCI-H209 cell	Growth inhibition assay	Inhibition of human NCI-H209 cell growth in a cell viability assay, IC50=0.1758 μM
human CTV-1 cell	Growth inhibition assay	Inhibition of human CTV-1 cell growth in a cell viability assay, IC50=0.18389 μM
LU-139 cell	Growth inhibition assay	Inhibition of human LU-139 cell growth in a cell viability assay, IC50=0.19435 μM
ML-2 cell	Growth inhibition assay	Inhibition of human ML-2 cell growth in a cell viability assay, IC50=0.22661 μM
human K5 cell	Growth inhibition assay	Inhibition of human K5 cell growth in a cell viability assay, IC50=0.22917 μM
human SBC-1 cell	Growth inhibition assay	Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=0.2362 μM
human COR-L88 cell	Growth inhibition assay	Inhibition of human COR-L88 cell growth in a cell viability assay, IC50=0.3348 μM
human KY821 cell	Growth inhibition assay	Inhibition of human KY821 cell growth in a cell viability assay, IC50=0.39603 μM
human HCC2218 cell	Growth inhibition assay	Inhibition of human HCC2218 cell growth in a cell viability assay, IC50=0.49728 μM
human ECC10 cell	Growth inhibition assay	Inhibition of human ECC10 cell growth in a cell viability assay, IC50=0.65389 μM
human EW-3 cell	Growth inhibition assay	Inhibition of human EW-3 cell growth in a cell viability assay, IC50=0.66611 μM
human EW-18 cell	Growth inhibition assay	Inhibition of human EW-18 cell growth in a cell viability assay, IC50=0.74679 μM
human UACC-257 cell	Growth inhibition assay	Inhibition of human UACC-257 cell growth in a cell viability assay, IC50=1.20326 μM
human G-361 cell	Growth inhibition assay	Inhibition of human G-361 cell growth in a cell viability assay, IC50=1.49519 μM
human HMV-II cell	Growth inhibition assay	Inhibition of human HMV-II cell growth in a cell viability assay, IC50=1.77184 μM
human DEL cell	Growth inhibition assay	Inhibition of human DEL cell growth in a cell viability assay, IC50=2.20704 μM
human IGROV-1 cell	Growth inhibition assay	Inhibition of human IGROV-1 cell growth in a cell viability assay, IC50=2.43188 μM
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
human LAMA-84 cell	Growth inhibition assay	Inhibition of human LAMA-84 cell growth in a cell viability assay, IC50=2.71284 μM
human NCI-H510A cell	Growth inhibition assay	Inhibition of human NCI-H510A cell growth in a cell viability assay, IC50=2.92526 μM
human CP66-MEL cell	Growth inhibition assay	Inhibition of human CP66-MEL cell growth in a cell viability assay, IC50=2.93559 μM
human HAL-01 cell	Growth inhibition assay	Inhibition of human HAL-01 cell growth in a cell viability assay, IC50=3.27918 μM
human RS4-11 cell	Growth inhibition assay	Inhibition of human RS4-11 cell growth in a cell viability assay, IC50=3.70573 μM
human RPMI-8226 cell	Growth inhibition assay	Inhibition of human RPMI-8226 cell growth in a cell viability assay, IC50=3.82376 μM
human NCI-H82 cell	Growth inhibition assay	Inhibition of human NCI-H82 cell growth in a cell viability assay, IC50=3.89305 μM
human NY cells	Growth inhibition assay	Inhibition of human NY cell growth in a cell viability assay, IC50=4.27637 μM
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
human MOLT-4 cell	Growth inhibition assay	Inhibition of human MOLT-4 cell growth in a cell viability assay, IC50=4.99193 μM
human DU-4475 cell	Growth inhibition assay	Inhibition of human DU-4475 cell growth in a cell viability assay, IC50=5.05565 μM
human ESS-1 cell	Growth inhibition assay	Inhibition of human ESS-1 cell growth in a cell viability assay, IC50=5.29179 μM
human NCI-H1299 cell	Growth inhibition assay	Inhibition of human NCI-H1299 cell growth in a cell viability assay, IC50=5.53033 μM
human COLO-684 cell	Growth inhibition assay	Inhibition of human COLO-684 cell growth in a cell viability assay, IC50=5.58165 μM
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
human D-542MG cell	Growth inhibition assay	Inhibition of human D-542MG cell growth in a cell viability assay, IC50=6.39272 μM
human A4-Fuk cell	Growth inhibition assay	Inhibition of human A4-Fuk cell growth in a cell viability assay, IC50=6.43662 μM
human HL-60 cell	Growth inhibition assay	Inhibition of human HL-60 cell growth in a cell viability assay, IC50=7.52212 μM
human NCI-H526 cell	Growth inhibition assay	Inhibition of human NCI-H526 cell growth in a cell viability assay, IC50=7.59801 μM
human L-363 cell	Growth inhibition assay	Inhibition of human L-363 cell growth in a cell viability assay, IC50=7.79252 μM
human A388 cell	Growth inhibition assay	Inhibition of human A388 cell growth in a cell viability assay, IC50=7.80384 μM
human MS-1	Growth inhibition assay	Inhibition of human MS-1 cell growth in a cell viability assay, IC50=7.83465 μM
human JAR cell	Growth inhibition assay	Inhibition of human JAR cell growth in a cell viability assay, IC50=7.84923 μM
human TI-73 cell	Growth inhibition assay	Inhibition of human TI-73 cell growth in a cell viability assay, IC50=8.0622 μM
human CTB-1 cell	Growth inhibition assay	Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=8.17825 μM
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
human HT-29 cell	Growth inhibition assay	Inhibition of human HT-29 cell growth in a cell viability assay, IC50=13.9111 μM
human NCI-H1092 cell	Growth inhibition assay	Inhibition of human NCI-H1092 cell growth in a cell viability assay, IC50=14.318 μM
human KMOE-2 cell	Growth inhibition assay	Inhibition of human KMOE-2 cell growth in a cell viability assay, IC50=14.6178 μM
human EM-2 cell	Growth inhibition assay	Inhibition of human EM-2 cell growth in a cell viability assay, IC50=15.2841 μM
human RT-112 cell	Growth inhibition assay	Inhibition of human RT-112 cell growth in a cell viability assay, IC50=15.3984 μM
human DB cell	Growth inhibition assay	Inhibition of human DB cell growth in a cell viability assay, IC50=15.8513 μM
human NCI-H1770 cell	Growth inhibition assay	Inhibition of human NCI-H1770 cell growth in a cell viability assay
human CAL-54 cell	Growth inhibition assay	Inhibition of human CAL-54 cell growth in a cell viability assay, IC50=16.73 μM
human NB14 cell	Growth inhibition assay	Inhibition of human NB14 cell growth in a cell viability assay, IC50=17.6395 μM
human RPMI-7951 cell	Growth inhibition assay	Inhibition of human RPMI-7951 cell growth in a cell viability assay, IC50=19.1783 μM
human T47D cell	Growth inhibition assay	Inhibition of human T47D cell growth in a cell viability assay, IC50=21.2243 μM
human A549 cell	Growth inhibition assay	Inhibition of human A549 cell growth in a cell viability assay, IC50=21.2811 μM
human A2780 cell	Growth inhibition assay	Inhibition of human A2780 cell growth in a cell viability assay, IC50=21.8225 μM
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
Cliquez pour voir plus de données expérimentales sur la lignée cellulaire

Informations chimiques, stockage et stabilité

Poids moléculaire	404.3	Formule	C₁₉H₁₂F₄N₄O₂	Stockage (À compter de la date de réception)	3 ans-20°Cpoudre
N° CAS	745833-23-2	Télécharger le SDF		Stockage des solutions mères	1 an-80°Cen solvant 1 mois-20°Cen solvant
Synonymes	N/A			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

Solubilité

In vitro
Lot:

DMSO : 81 mg/mL (200.34 mM)
(Le DMSO contaminé par lhumidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse	Concentration	Volume	Poids moléculaire
=	×	×

Calculateur de dilution Calculateur de poids moléculaire

In vivo Lot:
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 Validé par les laboratoires Selleck. Si vous avez besoin dajustements à cette formulation, contactez notre équipe commerciale pour des tests personnalisés.	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.

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant lexpérience)

Dosage : mg/kg Poids moyen des animaux : g Volume de dosage par animal :μL Nombre danimaux :

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter dabord sil ny a pas de formulation in vivo dans la section Solubilité.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter dabord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH₂O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant dajouter le solvant suivant.
2. Assurez-vous dajouter le(s) solvant(s) dans lordre. Vous devez vous assurer que la solution obtenue, lors de lajout précédent, est une solution claire avant de procéder à lajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme daction

Caractéristiques	Highly selective, orally active inhibitor of p38 MAPK.
Targets/IC₅₀/Ki	p38α (Cell-free assay) 4 nM-20 nM
In vitro	La pré-incubation des plaquettes avec du VX-702 (1 μM) inhibe complètement ou partiellement l'activation de la p38 (IC50 de 4 à 20 nM) induite par des agonistes plaquettaires incluant la thrombine, le SFLLRN, l'AYPGKF, l'U46619 et le collagène. Ce composé n'a aucun effet sur l'agrégation plaquettaire induite par l'un des agonistes de la p38 MAPK en présence ou en l'absence de thérapies antiplaquettaires. Il inhibe la production d'IL-6, d'IL-1β et de TNFα (IC50 = 59, 122 et 99 ng/mL, respectivement) de manière dose-dépendante.
In vivo	La demi-vie du VX-702 est de 16 à 20 heures, avec une clairance médiane de 3,75 L/h et un volume de distribution de 73 L/kg. Les valeurs d'AUC et de C_max sont proportionnelles à la dose pour ce composé, qui est principalement éliminé par voie rénale. Ce composé (à une dose de 0,1 mg/kg deux fois par jour) a un effet équivalent. De plus, cette substance chimique (5 mg/kg deux fois par jour), mesurée par le pourcentage d'inhibition de l'érosion des articulations du poignet et le score d'inflammation. Il inhibe sélectivement l'activation de la p38 MAPK après l'ischémie sans effet sur les ERKs et les JNKs. Le rapport IM/AAR est significativement réduit dans le groupe de 50 mg/kg par rapport aux groupes de 5 mg/kg et de véhicule.
Références	[1] https://pubmed.ncbi.nlm.nih.gov/15583748/ [2] http://eprints.utas.edu.au/3610/1/vx-702.pdf [3] http://eprints.utas.edu.au/3610/1/vx-702.pdf [4] http://circ.ahajournals.org/content/108/17.toc

Informations sur lessai clinique

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT	Recrutement	Conditions	Promoteur/Collaborateurs	Date de début	Phases
NCT00395577	Completed	Rheumatoid Arthritis	Vertex Pharmaceuticals Incorporated	November 2006	Phase 2

Support technique

Instructions de manipulation

Tel: +1-832-582-8158 Ext:3

Si vous avez dautres questions, veuillez laisser un message.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):