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VX-702 p38 MAPK inhibidor

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

Cat. No.S6005

VX-702 es un inhibidor altamente selectivo de p38α MAPK, con una potencia 14 veces mayor contra la p38α en comparación con la p38β.

VX-702 p38 MAPK inhibidor Chemical Structure

Estructura química

Peso molecular: 404.3

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Control de calidad

Lote: Pureza: 99.94%

99.94

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

Cultivo celular, tratamiento y concentración de trabajo

Líneas celulares	Tipo de ensayo	Descripción de la actividad
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
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Información química, almacenamiento y estabilidad

Peso molecular	404.3	Fórmula	C₁₉H₁₂F₄N₄O₂	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	745833-23-2	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	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

Solubilidad

In vitro
Lote:

DMSO : 81 mg/mL (200.34 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción

Características	Highly selective, orally active inhibitor of p38 MAPK.
Targets/IC₅₀/Ki	p38α (Cell-free assay) 4 nM-20 nM
In vitro	La preincubación de plaquetas con VX-702 (1 μM) inhibe completa o parcialmente la activación de p38 (IC50 de 4 a 20 nM) inducida por agonistas plaquetarios que incluyen trombina, SFLLRN, AYPGKF, U46619 y colágeno. Este compuesto no muestra ningún efecto sobre la agregación plaquetaria inducida por ninguno de los agonistas de p38 MAPK en presencia o ausencia de terapias antiplaquetarias. Inhibe la producción de IL-6, IL-1β y TNFα (IC50 = 59, 122 y 99 ng/mL, respectivamente) de manera dosis-dependiente.
In vivo	La semivida de VX-702 es de 16 a 20 horas, con una depuración media de 3,75 L/h y un volumen de distribución de 73 L/kg. Los valores de AUC y C_max son proporcionales a la dosis para este compuesto, que se elimina predominantemente por vía renal. Este compuesto (a una dosis de 0,1 mg/kg dos veces al día) tiene un efecto equivalente. Además, este químico (5 mg/kg dos veces al día), medido por el porcentaje de inhibición de la erosión de la articulación de la muñeca y la puntuación de inflamación. Inhibe selectivamente la activación de p38 MAPK después de la isquemia sin efectos sobre ERKs y JNKs. La relación IM/AAR se reduce significativamente en el grupo de 50 mg/kg en comparación con los grupos de 5 mg/kg y vehículo.
Referencias	[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

Información del ensayo clínico

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT00395577	Completed	Rheumatoid Arthritis	Vertex Pharmaceuticals Incorporated	November 2006	Phase 2

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