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

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.97%

99.97

Relaterade mål	CDK HSP PD-1/PD-L1 ROCK Wee1 DNA/RNA Synthesis Microtubule Associated Ras KRas Casein Kinase
Övrigt Aurora Kinase Inhibitorer	Hesperadin Alisertib (MLN8237) Tozasertib (VX-680, MK-0457) ZM 447439 MLN8054 Danusertib (PHA-739358) MK-5108 TCS7010 (Aurora A Inhibitor I) AMG-900 CCT137690

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Inkubationstid	Formulering	Aktivitetsbeskrivning	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
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	507.56	Formel	C₂₆H₃₀FN₇O₃	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	722544-51-6	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	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

Löslighet (Solubility)

In vitro
Batch:

DMSO : 100 mg/mL (197.02 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Targets/IC₅₀/Ki	Aurora B (Cell-free assay) 0.37 nM
In vitro	Barasertib (AZD1152-HQPA), a highly selective Aurora B inhibitor, causes polyploidy and apoptosis in many cancer cell lines.
In vivo	Barasertib (AZD1152-HQPA) is an aurora B kinase inhibitor, and has efficacy against RB1 / SCLC cell line xenografts, RB1 / SCLC PDXs, and autochthonous Rb1 / neuroendocrine tumors.
Referenser	[1] https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6368871/ [2] https://pubmed.ncbi.nlm.nih.gov/17495131/

Applikationer (Applications)

Metoder	Biomarkörer	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

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT02579226	Completed	Advanced Solid Tumours	AstraZeneca	October 28 2015	Phase 1

Vanliga frågor (Frequently Asked Questions)

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

Svar:
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.

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):

Barasertib-HQPA (AZD2811) Aurora B-hämmare

Molekylvikt: 507.56

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Vanliga frågor (Frequently Asked Questions)

Barasertib-HQPA (AZD2811) Aurora B-hämmare

Molekylvikt: 507.56

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Applikationer (Applications)

Klinisk prövningsinformation (Clinical Trial Information)

Vanliga frågor (Frequently Asked Questions)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)