Name: Barasertib-HQPA (AZD2811)
Brand: Selleck Chemicals
SKU: S1147
Rating: 5 (164 reviews)

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Batch: Zuiverheid: 99.97%

99.97

Gerelateerde doelwitten	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Casein Kinase
Overige Aurora Kinase Inhibitoren	Hesperadin Alisertib (MLN8237) Tozasertib (VX-680) ZM 447439 MLN8054 Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 PHA-680632

Celkweek, behandeling & werkconcentratie

Cellijnen	Assaytype	Concentratie	Incubatietijd	Formulering	Activiteitsbeschrijving	PMID
LNCaP	Growth Inhibition Assay	0-500 nM	48 h		IC50=25 nM	25277659
LNCaP	Apoptosis Assay	0-500 nM	48 h		induces apoptotic cell death through caspase-3 upregulation	25277659
LNCaP	Function Assay	50 nM	48 h		induces micronuclei with aneugenic mechanism	25277659
Ramos	Function Assay	500 nM	0-72 h		inhibits Aurora B kinase	21371446
Daudi	Function Assay	500 nM	0-72 h		inhibits Aurora B kinase	21371446
L540	Function Assay	500 nM	0-72 h		inhibits Aurora B kinase	21371446
BJAJ	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth significantly	21371446
Ramos	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth significantly	21371446
Raji	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth significantly	21371446
Daudi	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth significantly	21371446
L428	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth	21371446
KM-H2	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth	21371446
HDLM-2	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth	21371446
L450	Growth Inhibition Assay	500 nM	0-72 h		inhibits cell growth	21371446
BJAJ	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
Ramos	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
Raji	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
Daudi	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
L428	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
KM-H2	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
HDLM-2	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
L450	Apoptosis Assay	500 nM	0-72 h		induces apoptosis in a time-dependent manner	21371446
SW620	Growth Inhibition Assay				EC50=10±2.1 nM	21245090
HCT116	Growth Inhibition Assay				EC50=11±3.3 nM	21245090
MDA-MB-435	Growth Inhibition Assay	0-10000 nM	2-5 d	DMSO	IC50=125 nM	20175926
MDA-MB-468	Growth Inhibition Assay	0-10000 nM	2-5 d	DMSO	IC50=14 nM	20175926
MDA-MB-231	Growth Inhibition Assay	0-10000 nM	2-5 d	DMSO	IC50=105 nM	20175926
BT474	Growth Inhibition Assay	0-10000 nM	2-5 d	DMSO	IC50=8 nM	20175926
MDA-MB-361	Growth Inhibition Assay	0-10000 nM	2-5 d	DMSO	IC50=70 nM	20175926
HER18	Growth Inhibition Assay	0-10000 nM	2-5 d	DMSO	IC50=20 nM	20175926
HER18	Apoptosis Assay	100 nM	0/24/48 h	DMSO	induces apoptosis and reduces clonogenic potential	20175926
MDA-MB-231	Apoptosis Assay	105 nM	0/24/48 h	DMSO	induces apoptosis and reduces clonogenic potential	20175926
JHH-1	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=17.4±1.0 nM	19913935
JHH-2	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=218.0±10.8 nM	19913935
JHH-4	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=155.6±16.8 nM	19913935
HuH-1	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=27.3±5.0 nM	19913935
HuH-6	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=3.7±0.6 nM	19913935
HuH-7	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=6.8±0.3 nM	19913935
HLE	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=45.9±6.4 nM	19913935
HLF	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=126.1±12.2 nM	19913935
PLC/PRF/5	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=76.9±9.9 nM	19913935
SK-Hep1	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=21.9±1.2 nM	19913935
Hep3B	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=7.6±1.2 nM	19913935
HepG2	Growth Inhibition Assay	0.3–1000 nM	72 h		EC50=14.7±1.7 nM	19913935
Ramos	Apoptosis Assay	25/50/100 nM	48 h		increases the levels of the cleaved forms of PARP and caspase 3	19823168
Daudi	Apoptosis Assay	25/50/100 nM	48 h		increases the levels of the cleaved forms of PARP and caspase 3	19823168
BALM-14	Apoptosis Assay	12.5/25/50 nM	48 h		increases the levels of the cleaved forms of PARP and caspase 3	19823168
BALM-27	Apoptosis Assay	12.5/25/50 nM	48 h		increases the levels of the cleaved forms of PARP and caspase 3	19823168
NB4	Growth Inhibition Assay	0.01/0.1/1 μM	48 h		inhibits cell growth significantly	18367484
HeLa	Function Assay	1 uM	24 hrs		Inhibition of aurora B autophosphorylation in human HeLa cells at 1 uM after 24 hrs by Western blotting	20684549
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit

Moleculair gewicht	507.56	Formule	C₂₆H₃₀FN₇O₃	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	722544-51-6	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	AZD2811, INH-34, Barasertib-HQPA , Defosbarasertib			Smiles	CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO

Oplosbaarheid

In vitro
Batch:

DMSO : 100 mg/mL (197.02 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

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.
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.	5.000mg/ml (9.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 500 μL 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.	0.650mg/ml (1.28mM)	Taking the 1 mL working solution as an example, add 50 μL of 13 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.
Clear solution	5%DMSO 1 40%PEG 300 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.	2.500mg/ml (4.93mM)	Taking the 1 mL working solution as an example, add 50 μL of 50 mg/mL clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify; add 50 μL Tween-80 to the above system, mix evenly to clarify; Then continue to add 500 μL ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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

Targets/IC₅₀/Ki	Aurora B (Cell-free assay) 0.37 nM
In vitro	Barasertib (AZD1152-HQPA), een zeer selectieve Aurora B-remmer, veroorzaakt polyploïdie en apoptose in veel kankercellijnen.
In vivo	Barasertib (AZD1152-HQPA) is een Aurora B kinase-remmer en heeft werkzaamheid tegen RB1 / SCLC-zellijn-xenografts, RB1 / SCLC PDX'en en autochtone Rb1 / neuro-endocriene tumoren.
Referenties	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6368871/ [2] https://pubmed.ncbi.nlm.nih.gov/17495131/

Toepassingen

Methoden	Biomarkers	PMID
Western blot	AURKB / pSer10 Histone H3 / TP53 / CDKN1A / MYCN p53 / p21 / p-p38 / p38	26497213
Immunofluorescence	p21	24782314
Growth inhibition assay	Cell viability	26497213

Informatie klinische proef

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

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
NCT02579226	Completed	Advanced Solid Tumours	AstraZeneca	October 28 2015	Phase 1

Technische ondersteuning

Gebruiksaanwijzing

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

Als u nog andere vragen heeft, kunt u een bericht achterlaten.

Veelgestelde vragen

Vraag 1:
Can you let me know what solvent I can use for it, cat # S1147, for in vivo use? (IP injection in mice)

Antwoord:
S1147 can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30mg/ml as a clear solution. Usually, when prepare the solution, we will add organic solvents first, then add Tween 80, then water. But this compound can not dissolve in 30% PEG400/0.5% Tween80/5% Propylene glycol clearly. After water was added, it became a clear solution.

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Barasertib-HQPA (AZD2811) Aurora B-remmer

Chemische structuur

Moleculair gewicht: 507.56