Name: CYC116
Brand: Selleck Chemicals
SKU: S1171
Rating: 5 (12 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.52%

99.52

Gerelateerde doelwitten	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Casein Kinase
Overige Aurora Kinase Inhibitoren	Hesperadin Barasertib-HQPA (AZD2811) Alisertib (MLN8237) Tozasertib (VX-680, MK-0457) ZM 447439 MLN8054 Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Incubatietijd	Activiteitsbeschrijving
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by MTT assay
MIAPaCa2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MIAPaCa2 cells after 96 hrs by MTT assay
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by MTT assay
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by MTT assay
HeLa cells	Cytotoxicity assay		96 h	Cytotoxicity against human HeLa cells after 96 hrs by MTT assay
COLO205 cells	Cytotoxicity assay		96 h	Cytotoxicity against human COLO205 cells after 96 hrs by MTT assay
HCT116 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HCT116 cells after 96 hrs by MTT assay
K562 cells	Cytotoxicity assay		96 h	Cytotoxicity against human K562 cells after 96 hrs by MTT assay
CCRF-CEM cells	Cytotoxicity assay		96 h	Cytotoxicity against human CCRF-CEM cells after 96 hrs by MTT assay
MV4-11 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MV4-11 cells after 96 hrs by MTT assay
HL60 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HL60 cells after 96 hrs by MTT assay
NCI-H460 cells	Cytotoxicity assay		96 h	Cytotoxicity against human NCI-H460 cells after 96 hrs by MTT assay
MESSA cells	Cytotoxicity assay		96 h	Cytotoxicity against human MESSA cells after 96 hrs by MTT assay
U2OS cells	Function assay	0.07-10 uM	2 h	Inhibition of Aurora kinase in nocodazole-synchronized human U2OS cells assessed as reduction of histone H3 serine-10 phosphorylation at 0.07 to 10 uM after 2 hrs immunofluorescence microscopy
A549 cells	Function assay	0.5-2 μM	7 h	Cell cycle arrest in asynchronous human A549 cells assessed as accumulation of cyclin B1-negative tetraploid cells at G1 phase at 0.5 to 2 uM after 7 hrs by FACS analysis
SW620 cells	Function assay	1 μM	48 h	Effect on mitotic index in human SW620 cells assessed as appearance of polyploid cells at 1 uM after 48 hrs by propidium iodide staining-based FACS analysis
HeLa cells	Function assay	1.25 μM	7 h	Inhibition of Aurora kinase in human HeLa cells assessed as complete inhibition of histone H3 phosphorylation at 1.25 uM after 7 hrs by Western blot analysis
A549 cells	Function assay		7 h	Inhibition of Aurora kinase in human A549 cells assessed as concentration required for half-maximal inhibition of histone H3 serine-10 phosphorylation after 7 hrs immunofluorescence microscopy
BxPC3 cells	Cytotoxicity assay		96 h	Cytotoxicity against human BxPC3 cells after 96 hrs by MTT assay
HUPT4 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HUPT4 cells after 96 hrs by MTT assay
Saos2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human Saos2 cells after 96 hrs by MTT assay
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	368.46	Formule	C₁₈H₂₀N₆OS	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	693228-63-6	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	N/A			Smiles	CC1=C(SC(=N1)N)C2=NC(=NC=C2)NC3=CC=C(C=C3)N4CCOCC4

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 24 mg/mL (65.13 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

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Massa	Concentratie	Volume	Moleculair gewicht
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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.
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.	1.200mg/ml (3.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 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.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.200mg/ml (3.26mM)	Taking the 1 mL working solution as an example, add 50 μL of 24 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. 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.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van 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 het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

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

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

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. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Kenmerken	An orally bioavailable, small molecule inhibitor of Aurora kinase/VEGFR2.
Targets/IC₅₀/Ki	Aurora A (Cell-free assay) 8 nM(Ki) Aurora B (Cell-free assay) 9 nM(Ki) VEGFR2 (Cell-free assay) 44 nM(Ki) FLT3 (Cell-free assay) 44 nM(Ki) CDK2/CyclinE (Cell-free assay) 0.39 μM(Ki) CDK9/CyclinT (Cell-free assay) 0.48 μM(Ki) p70 S6K (Cell-free assay) 0.54 μM(Ki)
In vitro	The most Aurora-selective CYC116 shows inhibitory effect on Aurora A and B kinases 50-fold more potently than any of the CDKs assayed. This compound is initially screened against a panel of human leukemia and solid tumor cell lines using an MTT antiproliferative assay. The results show that it has broad-spectrum antitumor activity and shows specific cytotoxicity against the acute myelogenous leukemia cell line MV4-11 with IC50 of 34 nM. In addition, anti-proliferative activity of this chemical is found to be associated with Aurora A and B modulation such as, inhibition of Aurora autophosphorylation, reduction of histone H3 phosphorylation, polyploidy, followed by cell death, resulting from a failure in cytokinesis.
Kinase Assay	Kinase Assays
Kinase Assay	Aurora A kinase assays worden uitgevoerd met een reactievolume van 25 μL (25 mM β-glycerofosfaat, 20 mM Tris/HCl, pH 7,5, 5 mM EGTA, 1 mM DTT, 1 mM Na₃VO₄, 10 μg kemptide (peptide substraat)). Recombinant Aurora A kinase wordt verdund in 20 mM Tris/HCl, pH 8, met 0,5 mg/mL BSA, 2,5% glycerol en 0,006% Brij-35. Reacties worden gestart door toevoeging van 5 μL Mg/ATP-mix (15 mM MgCl₂, 100 μM ATP, met 18,5 kBq γ-³²P-ATP per putje) en geïncubeerd bij 30°C gedurende 30 minuten alvorens te stoppen met 25 μL 75 mM H₃PO₄. Aurora B kinase assays worden uitgevoerd zoals Aurora A, behalve dat Aurora B voorafgaand aan gebruik wordt geactiveerd in een aparte reactie bij 30°C gedurende 60 minuten met inner centromere protein.
In vivo	Mice bearing subcutaneous NCI-H460 xenografts are given CYC116 orally for 5 days, at dose levels of 75 and 100 mg/kg q.d. It leads to tumor growth delays of 2.3 and 5.8 days, which translated into specific growth delays of 0.32 and 0.81, respectively.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/20462263/

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2021-12-22)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT00560716	TERMINATED	Solid Tumors	Cyclacel Pharmaceuticals, Inc.	2007-06	PHASE1

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CYC116 Aurora Kinase Remmer

Moleculair gewicht: 368.46

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

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In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

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CYC116 Aurora Kinase Remmer

Moleculair gewicht: 368.46

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie klinische proef (Clinical Trial Information)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)