Name: Brequinar
Brand: Selleck Chemicals
SKU: S6626
Rating: 5 (10 reviews)

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Controllo Qualità

Lotto: Purezza: 99.93%

99.93

Target correlati	HSP Transferase P450 (e.g. CYP17) PDE phosphatase PPAR Vitamin Carbohydrate Metabolism Mitochondrial Metabolism Drug Metabolite
Altro Dehydrogenase Inibitori	Vorasidenib (AG-881) (R)-GNE-140 CPI-613 (Devimistat) Glycyrrhizin (Glycyrrhizic Acid, NSC 167409) Sodium Dichloroacetate (DCA) AGI-5198 Gossypol Acetate AGI-6780 Emodin NCT-503

Coltura cellulare, trattamento e concentrazione di lavoro

Linee cellulari	Tipo di saggio	Concentrazione	Tempo di incubazione	Descrizione dellattività	PMID
insect cells	Function assay			Inhibition of human recombinant DHODH expressed in baculovirus infected insect cells using dihydroorotate as substrate in presence of quinone by dichlorophenol-indophenol dye based assay, IC50=0.01μM	27994748
A549	Antiviral assay			Antiviral activity against Yellow fever virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM	31557612
A549	Antiviral assay			Antiviral activity against West Nile virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM	31557612
A549	Antiviral assay			Antiviral activity against Dengue virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM	31557612
A549	Antiviral assay			Antiviral activity against Western equine encephalomyelitis virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM	31557612
A549	Antiviral assay			Antiviral activity against Vesicular stomatitis virus infected in human A549 cells assessed as reduction in virus replication, EC50=0.078μM	31557612
Jurkat	Antiproliferative assay		72 hrs	Inhibition of cell proliferation of human Jurkat cells incubated for 72 hrs by Celltiter-Glo assay, IC50=0.2μM	26079043
MDCK	Antiviral assay		48 hrs	Antiviral activity against VSV infected in MDCK cells assessed as inhibition of VSV replication after 48 hrs by plaque assay, EC50=0.3μM	23930152
MDCK	Antiviral assay		48 hrs	Antiviral activity against influenza A virus A/WSN/33 (H0N1) infected in MDCK cells after 48 hrs by plaque assay, EC50=0.46μM	23930152
HL60	Antiproliferative assay		72 hrs	Antiproliferative activity against human HL60 cells after 72 hrs by MTT assay, IC50=0.544μM	29727569
HCT116	Antiproliferative assay		72 hrs	Antiproliferative activity against human HCT116 cells over-expressing DHODH after 72 hrs by MTT assay, IC50=0.679μM	29727569
Jurkat T	Antiproliferative assay		72 hrs	Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye-based fluorescence assay, IC50=0.91μM	29939742
Jurkat T	Antiproliferative assay		72 hrs	Antiproliferative activity against human Jurkat T cells assessed as DNA content after 72 hrs by Hoechst 33258 dye based fluorometric method, IC50=0.93μM	28235702
MIAPaCa2	Antiproliferative assay		72 hrs	Antiproliferative activity against human MIAPaCa2 cells after 72 hrs by MTT assay, IC50=1.69μM	29727569
Jurkat T	Cytotoxicity assay		72 hrs	Cytotoxicity against human Jurkat T cells assessed as compound concentration required to induce up to 30% cell death after 72 hrs by Hoechst 33258 dye based fluorometric method, Activity=45μM	28235702
Jurkat T	Cytotoxicity assay		72 hrs	Cytotoxicity against human Jurkat T cells assessed as compound concentration required to induce =>30% cell death after 72 hrs by CellTox green assay, Activity=48.2μM	29939742
HCT116	Growth inhibition assay		72 hrs	Growth inhibition of human HCT116 cells over-expressing DHODH at 2 times antiproliferative IC50 after 72 hrs in absence of uridine by MTT assay	29727569
HCT116	Cytostatic activity assay	10 uM	24 hrs	Cytostatic activity against human HCT116 cells assessed as reduction in colony forming at 10 uM after 24 hrs by crystal violet staining based assay	29727569
HCT116	Cytostatic activity assay	10 uM	7 days	Cytostatic activity against human HCT116 cells assessed as reduction in colony forming at 10 uM after 7 days by crystal violet staining based assay	29727569
U937	Antiproliferative assay	0.01 to 10 uM	3 days	Antiproliferative activity against CFSE-labeled human U937 cells at 0.01 to 10 uM after 3 days by propidium iodide staining-based flow cytometry	29939742
THP1	Antiproliferative assay	0.01 to 10 uM	3 days	Antiproliferative activity against CFSE-labeled human THP1 cells at 0.01 to 10 uM after 3 days by propidium iodide staining-based flow cytometry	29939742
U937	Function assay	0.1 to 10 uM	up to 4 days	Induction of myeloid differentiation in human U937 cells assessed as increase in CD11b expression level at 0.1 to 10 uM up to 4 days by propidium iodide staining-based flow cytometry	29939742
THP1	Function assay	0.1 to 10 uM	up to 5 days	Induction of myeloid differentiation in human THP1 cells assessed as increase in CD11b expression level at 0.1 to 10 uM up to 5 days by propidium iodide staining-based flow cytometry	29939742
THP1	Function assay	0.1 to 10 uM	up to 5 days	Induction of myeloid differentiation in human THP1 cells assessed as increase in CD14 expression level at 0.1 to 10 uM up to 5 days by propidium iodide staining-based flow cytometry	29939742
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Informazioni chimiche, conservazione e stabilità

Peso molecolare	375.37	Formula	C₂₃H₁₅F₂NO₂	Conservazione (Dalla data di ricezione)	3 years -20°C powder
N. CAS	96187-53-0	--		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	DUP785, NSC 368390			Smiles	CC1=C(C2=C(C=CC(=C2)F)N=C1C3=CC=C(C=C3)C4=CC=CC=C4F)C(=O)O

Solubilità

In vitro
Lotto:

DMSO : 37 mg/mL (98.56 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : 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.
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	0.500mg/ml (1.33mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 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 it; 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.

Calcolatore di formulazione in vivo (Soluzione chiara)

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

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 cè 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, nellaggiunta precedente, sia una soluzione limpida prima di procedere allaggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno dacqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo dazione

Targets/IC₅₀/Ki	DHODH 20 nM
In vitro	Il Brequinar sodico (BQR) riduce i livelli di PyN nelle cellule T stimolate da Con A e l'inibizione della proliferazione cellulare a basse concentrazioni, che può essere invertita dall'uridina. Tuttavia, l'uridina non è in grado di invertire gli effetti di alte concentrazioni di BQR. Il BQR possiede la capacità di inibire la fosforilazione della tirosina.
In vivo	Il Brequinar sodico (BQR) induce anemia attraverso l'inibizione dell'attività della DHO-DHase e della sintesi de novo delle pirimidine in vivo. La co-somministrazione di BQR con uridina previene l'anemia.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/27641501/ [2] https://pubmed.ncbi.nlm.nih.gov/9551920/

Informazioni sullo studio clinico

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

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
NCT03760666	Terminated	Acute Myeloid Leukemia	Clear Creek Bio Inc.	December 20 2018	Phase 1\|Phase 2

Supporto tecnico

Istruzioni per la manipolazione

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

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Brequinar Dehydrogenase inibitore

Struttura chimica

Peso molecolare: 375.37