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

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.94%

99.94

Target correlati	EGFR VEGFR JAK FGFR PDGFR Src HIF HER2 FLT3 FLT
Altro VDA Inibitori	Plinabulin

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dell'attività	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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	282.29	Formula	C₁₇H₁₄O₄	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	117570-53-3	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	ASA404, NSC 640488			Smiles	CC1=C(C2=C(C=C1)C(=O)C3=CC=CC(=C3O2)CC(=O)O)C

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 16 mg/mL (56.67 mM) Riscaldato con bagno d'acqua a 60°C; Sonicato;
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

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

Water : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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.
Saggio chinasico	Attività della DT-diaphorase e analisi cinetica dell'inibizione enzimatica
Saggio chinasico	L'attività dell'enzima DT-diaphorase purificata viene saggiata misurando la riduzione del citocromo c a 550 nm su uno spettrofotometro Beckman DU 650. Ogni saggio contiene citocromo c (70 μM), NADH (concentrazioni variabili), DT-diaphorase purificata (0,032 μg) e menadione (concentrazioni variabili) in un volume finale di 1 mL di tampone Tris–HCl (50 mM, pH 7,4) contenente 0,14% di BSA. La reazione viene avviata con l'aggiunta di NADH. I tassi di riduzione vengono calcolati sulla parte iniziale della curva di reazione (30 secondi) e i risultati sono espressi in termini di μmol di citocromo c ridotto/min/mg di proteina utilizzando un coefficiente di estinzione molare di 21,1 mM⁻¹ cm⁻¹ per il citocromo c ridotto. I saggi enzimatici vengono eseguiti a temperatura ambiente e tutte le reazioni sono eseguite in triplicato. L'inibizione dell'attività della DT-diaphorase purificata viene eseguita includendo Vadimezan (DMXAA) a varie concentrazioni nella reazione, e le caratteristiche di inibizione sono determinate variando la concentrazione di NADH (menadione costante) o menadione (NADH costante) a diverse concentrazioni di questo composto. I valori di K_i si ottengono tracciando 1/V contro. L'attività della DT-diaphorase nelle cellule DLD-1 è determinata misurando la riduzione dicumarolo-sensibile del DCPIP a 600 nm. Brevemente, le cellule DLD-1 in fase di crescita esponenziale media vengono raccolte per raschiamento in tampone freddo (Tris–HCl, 25 mM, pH 7,4 e 250 mM saccarosio) e sonicato su ghiaccio. Le condizioni del saggio enzimatico sono 2 mM NADH, 40 μM DCPIP, 20 μL di dicumarolo (quando richiesto) in un volume finale di 1 mL di Tris–HCl (25 mM, pH 7,4) contenente BSA (0,7 mg/mL). I risultati sono espressi come la riduzione dicumarolo-sensibile del DCPIP utilizzando un coefficiente di estinzione molare di 21 mM⁻¹ cm⁻¹. I livelli di proteine sono determinati utilizzando il saggio di 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.
Riferimenti	[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/

Applicazioni (Applications)

Metodi	Biomarcatori	Immagini	PMID
Western blot	p-p38 / p38 p-MK2 / pERK / p-JNK		21819972
Growth inhibition assay	Cell proliferation		30138430

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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 Disruptore Vascolare

Peso molecolare: 282.29

Controllo Qualità (Quality Control)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Applicazioni (Applications)

Informazioni sullo studio clinico (Clinical Trial Information)

Vadimezan (DMXAA) Agente Disruptore Vascolare

Peso molecolare: 282.29

Controllo Qualità (Quality Control)

Coltura cellulare, trattamento e concentrazione di lavoro (Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Applicazioni (Applications)

Informazioni sullo studio clinico (Clinical Trial Information)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)