Barasertib-HQPA (AZD2811)

Catalogusnr.S1147 Batch:S114709

Afdrukken

Technische gegevens

Formule

C26H30FN7O3
Molecuulgewicht 507.56 CAS-nr. 722544-51-6
Oplosbaarheid (25°C)* In vitro DMSO 100 mg/mL (197.02 mM)
Water Insoluble
Ethanol Insoluble
In Vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
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 40%PEG300 5%Tween80 50%ddH2O

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 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 95% corn oil

Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor maatwerktesten.

 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. 
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving Defosbarasertib (AZD1152-HQPA, AZD2811, INH-34, Barasertib-HQPA) is een zeer selectieve Aurora B-remmer met een IC50 van 0,37 nM in een celvrije assay, ~3700 keer selectiever voor Aurora B dan voor Aurora A. Fase 1.
Doelen
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.

Protocol (uit referentie)

Celassay:

[1]
  • Cellijnen

    NCI-H82 cells, SCLC and NSCLC cell lines

  • Concentraties

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  • Incubatietijd

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  • Methode

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Referenties

  • https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6368871/
  • https://pubmed.ncbi.nlm.nih.gov/17495131/

Klantproductvalidatie

Targeting PI3K, a common downstream effector of RTKs, with a selective inhibitor (GDC0941) sensitizes SOX10 knockdown cells to vemurafenib. shRNAs targeting SOX10 were introduced into A375 cells by lentiviral transduction. pLKO.1 empty vector served as a control vector (Ctrl). Cells were seeded in 6-well plates at the same density in the presence or absence of drug(s) at the indicated concentration. Cells were cultured for 2 weeks in the absence of vemurafenib or 4 weeks in the presence of vemurafenib before fixing and staining.

Gegevens van [ Nature , 2014 , 508(7494), 118-22 ]

Primary MKPs were treated with the Aurora B inhibitor AZD-1152, and then stimulated with 20 ng/ml TPO for 5 d. Cell morphology was analyzed by Giemsa staining (Bar, 20 祄; red arrows denote mature MKs; n = 6).

Gegevens van [ J Exp Med , 2014 , 10.1084/jem.20141123 ]

<p>: Barasertib inhibits AURKB specifically and triggers mitotic slippage. (a) Barasertib inhibits AURKB without affecting AURKA. Mitotic HeLa cells were obtained by exposure to nocodazole for 16 h followed by mechanical shake off. The cells were incubated with the indicated concentrations of Barasertib for 2 h. Nocodazole and MG132 were included to prevent mitotic exit. Lysates were prepared and analyzed with immunoblotting. Uniform loading was confirmed by immunoblotting for actin. (b) Barasertib induces mitotic slippage. HeLa cells expressing histone H2B-GFP were exposed to buffer or the indicated concentrations of Barasertib. Individual cells were then tracked for 24 h with time- lapse microscopy. Each horizontal bar represents one cell (n ¼ 50). The key is the same as in Figure 1b. (c) Summary of Barasertib-mediated mitotic slippage. Live-cell imaging after Barasertib treatment was described in panel (b). The duration of mitosis (mean±90% confidence interval) and the percentage of cells that underwent mitotic slippage during the imaging period were quantified. (d) Genome reduplication after Barasertib-mediated mitotic slippage. HeLa cells were treated with the indicated concentrations of Barasertib for 36 h. DNA contents were analyzed with flow cytometry. (e) Barasertib induces mitotic slippage and genome reduplication in HCT116. Cells were treated with the indicated concentrations of Barasertib for 24 h. DNA contents were analyzed with flow cytometry. (f) Cytotoxicity induced by Barasertib. HeLa and HCT116 cells were cultured in the presence of the indicated concentrations of Barasertib for 48 h. Proliferation was assayed with WST-1 assay. (g) Barasertib induces genome reduplication and apoptosis. HeLa cells were incubated with 50 n M of Barasertib either in the presence or absence of the caspase inhibitor Z-VAD(OMe)-FMK. The cells were harvested at the indicated time points and analyzed with flow cytometry.</p>

Gegevens van [ Oncogene , 2014 , 33, 3550-60 ]

<p> </p><p>Dual inhibition of Aurora and SRC kinases specifically eliminates hyperploid cells. Experiment shown is same as a, b, but performed following treatment of OVCAR10 cells with MLN8237 (targeting AURKA) or AZD1152 (targeting AURKB);</p>

Gegevens van [ Oncogene , 2012 , 31, 1217–1227 ]

Sellecks Barasertib-HQPA (AZD2811) Is geciteerd door 171 Publicaties

High-throughput screening identifies Aurora kinase B as a critical therapeutic target for Merkel cell carcinoma [ Nat Commun, 2025, 16(1):1583] PubMed: 39939315
Unraveling AURKB as a potential therapeutic target in pulmonary hypertension using integrated transcriptomic analysis and pre-clinical studies [ Cell Rep Med, 2025, 6(2):101964] PubMed: 39933527
Aurora B controls microtubule stability to regulate abscission dynamics in stem cells [ Cell Rep, 2025, 44(2):115238] PubMed: 39854207
Identification of chemical inhibitors targeting long noncoding RNA through gene signature-based high throughput screening [ Int J Biol Macromol, 2025, 292:139119] PubMed: 39722392
Oversized cells activate global proteasome-mediated protein degradation to maintain cell size homeostasis [ Elife, 2025, 14e75393] PubMed: 39791360
The mechanoresponsive chromosomal passenger complex sustains furrow ingression under confinement [ J Mol Cell Biol, 2025, mjaf019] PubMed: 40693957
Overcoming MET-targeted drug resistance in MET-amplified lung cancer by aurora kinase B inhibition [ Biochim Biophys Acta Mol Cell Res, 2025, 1872(7):120001] PubMed: 40499687
Proteomic profiling identifies upregulation of aurora kinases causing resistance to taxane-type chemotherapy in triple negative breast cancer [ Sci Rep, 2025, 15(1):3211] PubMed: 39863788
Nucleosome stability safeguards cell identity, stress resilience and healthy aging [ bioRxiv, 2025, 2025.09.17.676776] PubMed: 41000743
Proteogenomic characterization of small cell lung cancer identifies biological insights and subtype-specific therapeutic strategies [ Cell, 2024, 187(1):184-203.e28] PubMed: 38181741

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.