Name: Vadimezan (DMXAA)
Brand: Selleck Chemicals
SKU: S1537
Rating: 5 (45 reviews)

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Control de calidad (Quality Control)

Lote: Pureza: 99.94%

99.94

Dianas relacionadas	EGFR VEGFR JAK FGFR PDGFR Src HIF HER2 FLT3 FLT
Otros VDA Inhibidores	Plinabulin

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Tiempo de incubación	Descripción de la actividad	PMID
human BJ cells	Cytotoxic assay		24 h	Cytotoxicity against human BJ cells after 24 hrs by MTT assay, CC50=48.9 μM	24518295
HECPP cells	Function assay	10 ug/mL		Activation of NF-kappaB in HECPP cells at 10 ug/mL	17616114
MCF7	Antiproliferative assay		24 hrs	Antiproliferative activity against human MCF7 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 11.89 μM.	29129511
MDA-MB-231	Antiproliferative assay		24 hrs	Antiproliferative activity against human MDA-MB-231 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 12.12 μM.	29129511
K562	Antiproliferative assay		24 hrs	Antiproliferative activity against human K562 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 19.14 μM.	29129511
HepG2	Antiproliferative assay		24 hrs	Antiproliferative activity against human HepG2 cells co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by MTT assay, IC50 = 21.25 μM.	29129511
COLO320	Antiproliferative assay		48 hrs	Antiproliferative activity against human COLO320 cells after 48 hrs by CCK8 assay, IC50 = 39.5 μM.	28376372
MDA-MB-231	Antiproliferative assay		48 hrs	Antiproliferative activity against human MDA-MB-231 cells after 48 hrs by CCK8 assay, IC50 = 48.4 μM.	28376372
MDA-MB-231	Growth inhibition assay		24 hrs	Growth inhibition of human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 48.42 μM.	29609121
MDA-MB-231	Antiproliferative assay		24 hrs	Antiproliferative activity against human MDA-MB-231 cells after 24 hrs by MTT assay, IC50 = 48.44 μM.	29129511
A673	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
DAOY	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells	29435139
RD	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells	29435139
SK-N-SH	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells	29435139
MG 63 (6-TG R)	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells	29435139
NB1643	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells	29435139
Rh41	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells	29435139
SK-N-MC	qHTS assay			qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells	29435139
MDA-MB-231	Apoptosis assay	24 to 96 uM	48 hrs	Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved caspase-3 expression at 24 to 96 uM after 48 hrs by Western blot analysis	28376372
MDA-MB-231	Apoptosis assay	24 to 96 uM	48 hrs	Induction of apoptosis in human MDA-MB-231 cells assessed as increase in cleaved PARP level at 24 to 96 uM after 48 hrs by Western blot analysis	28376372
MDA-MB-231	Function assay	24 to 96 uM	48 hrs	Decrease in caspase-3 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis	28376372
MDA-MB-231	Function assay	24 to 96 uM	48 hrs	Increase in p53 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis	28376372
MDA-MB-231	Function assay	24 to 96 uM	48 hrs	Decrease in caspase-9 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis	28376372
MDA-MB-231	Function assay	24 to 96 uM	48 hrs	Decrease in MDM2 level in human MDA-MB-231 cells at 24 to 96 uM after 48 hrs by Western blot analysis	28376372
HepG2	Cell cycle arrest assay	0.2 uM	24 hrs	Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase at 0.2 uM after 24 hrs by propidium iodide staining-based flow cytometric method relative to control	29129511
HepG2	Cell cycle arrest assay		24 hrs	Cell cycle arrest in human HepG2 cells assessed as accumulation at S phase co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by propidium iodide staining-based flow cytometric method	29129511
HepG2	Apoptosis assay	0.2 uM	24 hrs	Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 levels at 0.2 uM after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay	0.2 uM	24 hrs	Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-9 levels at 0.2 uM after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay		24 hrs	Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay	0.2 uM	24 hrs	Induction of apoptosis in human HepG2 cells assessed as increase in cleaved PARP levels at 0.2 uM after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay		24 hrs	Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-3 levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay		24 hrs	Induction of apoptosis in human HepG2 cells assessed as increase in cleaved caspase-9 levels co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay		24 hrs	Induction of apoptosis in human HepG2 cells assessed as downregulation of Bcl-xL expression co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method	29129511
HepG2	Apoptosis assay		24 hrs	Induction of apoptosis in human HepG2 cells assessed as upregulation of Bid expression co-treated with pyranoxanthone at 1:1 molar ratio after 24 hrs by Western blot method	29129511
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	282.29	Fórmula	C₁₇H₁₄O₄	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	117570-53-3	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	ASA404, NSC 640488			Smiles	CC1=C(C2=C(C=C1)C(=O)C3=CC=CC(=C3O2)CC(=O)O)C

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 16 mg/mL (56.67 mM) Calentado con baño de agua a 60°C; Ultrasonido;
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

7.5%Sodium bicarbonate : 10 mg/mL (Ultrasonic and heating for 5 minutes.)

Water : 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.
Clear solution	7.5% sodium bicarbonate Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	10.000mg/ml (35.42mM)	Dissolve 10 mg of the product in 1 ml of 7.5% Sodium bicarbonate (7.5% sodium bicarbonate solution), and heat with ultrasonic for five minutes until the solution becomes clear.
Clear solution	10%DMSO 1 40%PEG300 2 5%TWEEN80 3 45%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	1.600mg/ml (5.67mM)	Taking the 1 mL working solution as an example, add 100 μL of 16 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 450 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.
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	8% DMSO 1 40% PEG 300 2 5%Tween80 3 47% water Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	0.240mg/ml (0.85mM)	Taking the 1 mL working solution as an example, add 80 μL of 3mg/ml clear 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 it; then continue adding Dilute 470 μL ddH2O 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.
Clear solution	10% DMSO 1 40%PEG300 2 5%Tween80 3 45%ddH2O Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	0.750mg/ml (2.66mM)	Taking the 1 mL working solution as an example, add 100 μL of 7.5 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 450 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 (Mechanism of Action)

Targets/IC₅₀/Ki	DT-diaphorase (Cell-free assay) 20 μM(Ki) DT-diaphorase (Cell-free assay) 20 μM(Ki)
In vitro	In DLD-1 human colon carcinoma cells, Vadimezan (DMXAA) inhibits DT-diaphorase activity without significant effects on the activity of cytochrome b5 reductase and cytochrome P450 reductase. Combination of menadione and this compound leads to an increase in the antiproliferative activity of DLD-1 cells. As an antiviral agent, it inhibits VSV-induced cytotoxicity and influenza virus replication in RAW 264.7 macrophages. A recent study shows that DMXAA has non-immune-mediated inhibitory effects against several kinase members of VEGFR (vascular endothelial growth factor receptor), such as VEGFR2 signalling in human umbilical vein endothelial cells.
Ensayo de quinasa	Actividad de la DT-diaforasa y análisis cinético de la inhibición enzimática
Ensayo de quinasa	La actividad de la enzima DT-diaforasa purificada se ensaya midiendo la reducción del citocromo c a 550 nm en un espectrofotómetro Beckman DU 650. Cada ensayo contiene citocromo c (70 μM), NADH (concentraciones variables), DT-diaforasa purificada (0,032 μg) y menadiona (concentraciones variables) en un volumen final de 1 mL de tampón Tris–HCl (50 mM, pH 7,4) que contiene 0,14 % de BSA. La reacción se inicia con la adición de NADH. Las tasas de reducción se calculan sobre la parte inicial de la curva de reacción (30 segundos), y los resultados se expresan en términos de μmol de citocromo c reducido/min/mg de proteína utilizando un coeficiente de extinción molar de 21,1 mM⁻¹ cm⁻¹ para el citocromo c reducido. Los ensayos enzimáticos se llevan a cabo a temperatura ambiente y todas las reacciones se realizan por triplicado. La inhibición de la actividad de la DT-diaforasa purificada se realiza mediante la inclusión de Vadimezan (DMXAA) a varias concentraciones en la reacción, y las características de inhibición se determinan variando la concentración de NADH (menadiona constante) o menadiona (NADH constante) a varias concentraciones de este compuesto. Los valores de K_i se obtienen trazando 1/V frente a. La actividad de la DT-diaforasa en células DLD-1 se determina midiendo la reducción sensible al dicumarol de DCPIP a 600 nm. Brevemente, las células DLD-1 en crecimiento exponencial medio se cosechan raspando en tampón frío (Tris–HCl, 25 mM, pH 7,4 y 250 mM de sacarosa) y se sonicaron en hielo. Las condiciones del ensayo enzimático son 2 mM de NADH, 40 μM de DCPIP, 20 μL de dicumarol (cuando sea necesario) en un volumen final de 1 mL de Tris–HCl (25 mM, pH 7,4) que contiene BSA (0,7 mg/mL). Los resultados se expresan como la reducción de DCPIP sensible al dicumarol utilizando un coeficiente de extinción molar de 21 mM⁻¹ cm⁻¹. Los niveles de proteína se determinan utilizando el ensayo de Bradford.
In vivo	Vadimezan (DMXAA) treatment significantly protects C57BL/6J mice infected i.n. with 200 p.f.u. mouse-adapted H1N1 influenza PR8 virus with 60% survival, while the control group only exhibited 20% survival. This compound significantly delays tumor growth induced by chemical carcinogen, increases the time to tumor doubling and increases time from treatment to euthanasia. After its treatment, median tumor doubling time, median tumour tripling time and median time from treatment to euthanasia in tumor-bearing animals are increased by approximately 4.4-, 1.8- and 2.7-fold, respectively.
Referencias	[1] https://pubmed.ncbi.nlm.nih.gov/10423172/ [2] https://pubmed.ncbi.nlm.nih.gov/21084628/ [3] https://pubmed.ncbi.nlm.nih.gov/22142330/ [4] https://pubmed.ncbi.nlm.nih.gov/16944150/

Aplicaciones (Applications)

Métodos	Biomarcadores	Imágenes	PMID
Western blot	p-p38 / p38 p-MK2 / pERK / p-JNK		21819972
Growth inhibition assay	Cell proliferation		30138430

Información del ensayo clínico (Clinical Trial Information)

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

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
NCT00856336	Completed	Refractory Tumors	Antisoma Research	May 2003	Phase 1
NCT00863733	Completed	Solid Tumors	Cancer Research UK\|Cancer Society Auckland	May 1996	Phase 1

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):

Vadimezan (DMXAA) Agente Disruptor Vascular

Peso molecular: 282.29

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Información del ensayo clínico (Clinical Trial Information)

Vadimezan (DMXAA) Agente Disruptor Vascular

Peso molecular: 282.29

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Aplicaciones (Applications)

Información del ensayo clínico (Clinical Trial Information)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)