Name: Deferasirox (ICL670)
Brand: Selleck Chemicals
SKU: S1712
Rating: 5 (17 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.95%

99.95

Gerelateerde doelwitten	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease DPP
Overig P450 (e.g. CYP17) Inhibitoren	Apigenin Baicalein Naringenin Diosmetin Alizarin Orteronel Benzbromarone Sodium Danshensu Naringin Piperine

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving	PMID
MDA-MB-231	Cytotoxicity assay	96 hrs	Cytotoxicity against human MDA-MB-231 cells after 96 hrs by MTT assay, IC50=4μM	20005708
MIAPaCa2	Cytotoxicity assay	96 hrs	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay, IC50=10μM	20005708
SK-N-MC	Toxicity assay		Toxicity in human SK-N-MC cells by MTT method, IC50=20.54μM	20041672
Sf9	Function assay	20 mins	Inhibition of human MRP4 overexpressed in Sf9 cell membrane vesicles assessed as uptake of [3H]-estradiol-17beta-D-glucuronide in presence of ATP and GSH measured after 20 mins by membrane vesicle transport assay, IC50=36.5μM	23956101
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
NB-EBc1	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells	29435139
OHS-50	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells	29435139
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht	373.36	Formule	C₂₁H₁₅N₃O₄	Opslag (vanaf de datum van ontvangst)	3 jaar-20°Cpoeder
CAS-nr.	201530-41-8	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	CGP-72670, ICL-670			Smiles	C1=CC=C(C(=C1)C2=NN(C(=N2)C3=CC=CC=C3O)C4=CC=C(C=C4)C(=O)O)O

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 75 mg/mL (200.87 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Ethanol : 2 mg/mL

Water : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Molecuulgewicht
=	×	×

Verdunningscalculator Molecuulgewichtcalculator

In vivo Batch:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	3.700mg/ml (9.91mM)	Taking the 1 mL working solution as an example, add 50 μL of clarified DMSO stock solution of 74 mg/ml 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.
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.

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in de sectie oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-moedervloeistof: mg geneesmiddel vooropgelost in μL DMSO ( Concentratie moedervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de batch van het geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH₂O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

In vitro	Deferasirox effectively chelates iron from Rhizopus oryzae and demonstrates cidal activity in vitro against 28 of 29 clinical isolates of Mucorales at concentrations well below clinically achievable serum levels. This compound incubation induces a significant inhibition of NF-κB activity and a cytoplasmic sequestration of its active subunit p65 in an inactive form in 28 of 40 peripheral blood samples. It inhibits three human myeloid cell lines (K562, U937, and HL60) with IC50 of 17-50 mM. The chemical is cidal in vitro against A. fumigatus, with an MIC and MFC of 25 and 50 mg/L, respectively.
In vivo	Deferasirox significantly improves survival and decreased tissue fungal burden in diabetic ketoacidotic or neutropenic mice with mucormycosis, with an efficacy similar to that of liposomal amphotericin B. This compound treatment also enhances the host inflammatory response to mucormycosis. It synergistically improves survival and reduces tissue fungal burden when combined with liposomal amphotericin B. This chemical administered p.o. to rats is absorbed to at least 75%, and the bioavailability is 26%. It is present in the blood circulation mainly in the unchanged form and as its iron complex, Fe(deferasirox)2, after intravenous and p.o. administration. The compound is 99.2% bound to plasma proteins. It monotherapy modestly prolongs survival of mice with IPA.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/17786247/ [2] https://pubmed.ncbi.nlm.nih.gov/20534700/ [3] https://pubmed.ncbi.nlm.nih.gov/19298223/ [4] https://pubmed.ncbi.nlm.nih.gov/18775980/ [5] https://pubmed.ncbi.nlm.nih.gov/19942619/

Toepassingen (Applications)

Methoden	Biomarkers	PMID
Western blot	CDK2 / CDK4 / CDK6 / Cyclin A / Cyclin B / Cyclin D1 / Cyclin E / p53 / p27 / p21 TFR1 / Ferroportin Pro-caspase-3 / Pro-caspase-8 / Pro-caspase-9 / BAX / NDRG1 / c-Myc / p-mTOR	26965928
Immunofluorescence	Bax / TOM22 Cytochrome c	28139717
Growth inhibition assay	Cell viability Cell viability	26965928

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
NCT04423237	Recruiting	Iron Overload	University of Pisa\|IRCCS Burlo Garofolo\|University of Genova	September 30 2020	--
NCT03920657	Terminated	Myelodysplastic Syndromes	Fondazione Italiana Sindromi Mielodisplastiche-ETS	October 4 2019	Phase 2
NCT03372083	Completed	Iron Overload	Novartis Pharmaceuticals\|Novartis	January 16 2018	Phase 4
NCT02663752	Terminated	Myelodysplastic Syndrome	Novartis Pharmaceuticals\|Novartis	May 30 2016	Phase 2

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Deferasirox (ICL670) CYP1A2-remmer

Molecuulgewicht: 373.36

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Deferasirox (ICL670) CYP1A2-remmer

Molecuulgewicht: 373.36

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkzame concentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Toepassingen (Applications)

Informatie over klinische proeven (Clinical Trial Information)

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)