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Merck

SML0268

Sigma-Aldrich

AZD1152-HQPA

≥98% (HPLC)

Szinonimák:

3-[[7-[3-[Ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino]-N-(3-fluorophenyl)-1H-pyrazole-5-acetamide

Bejelentkezésa Szervezeti és Szerződéses árazás megtekintéséhez


About This Item

Tapasztalati képlet (Hill-képlet):
C26H30FN7O3
CAS-szám:
Molekulatömeg:
507.56
MDL-szám:
UNSPSC kód:
12352200
PubChem Substance ID:
NACRES:
NA.77

Minőségi szint

Teszt

≥98% (HPLC)

Forma

powder

szín

white to beige

oldhatóság

DMSO: >15 mg/mL

tárolási hőmérséklet

2-8°C

SMILES string

CCN(CCO)CCCOc1ccc2c(Nc3cc(CC(=O)Nc4cccc(F)c4)[nH]n3)ncnc2c1

InChI

1S/C26H30FN7O3/c1-2-34(10-11-35)9-4-12-37-21-7-8-22-23(16-21)28-17-29-26(22)31-24-14-20(32-33-24)15-25(36)30-19-6-3-5-18(27)13-19/h3,5-8,13-14,16-17,35H,2,4,9-12,15H2,1H3,(H,30,36)(H2,28,29,31,32,33)

Nemzetközi kémiai azonosító kulcs

QYZOGCMHVIGURT-UHFFFAOYSA-N

Alkalmazás

AZD1152-HQPA has been used as a specific inhibitor of aurora kinase B (AURKB) to examine the cell cycle stage the IRG (hit compound that induces an irregular nuclear shape)-treated cells accumulate and become senescent and also to study the roles of cyclin-dependent kinase 6 (CDK6) and AURKB in restricting enterovirus 71 (EV71) infection.
AZD1152-HQPA has been used:
  • for the dose dependent inhibition of aurora kinase B (AURKB)
  • as a component to identify that, replication timing regulatory factor 1 (RIF1) and protein phosphatase 1 (PP1) are critical for the regulation of abscission timing in human cells
  • as a component to study the relevance of AURKB as a cancer therapeutic target

Biokémiai/fiziológiai hatások

AZD1152-HQPA is a selective aurora-B kinase inhibitor; anti-cancer agent.
AZD1152-HQPA is the active metabolite of AZD-1152, a potent selective Aurora Kinase B inhibitor. AZD1152 is 50-fold selective for Aurora kinase B over Aurora kinase C and over 1000-fold selective for Aurora kinase B over Aurora Kinase A. (IC50s: aurora-A, 1,369 nmol/L; aurora-B, 0.36 nmol/L; aurora-C, 17.0 nmol/L). It is converted in plasma to the active form AZD1152-HQPA, which has been shown to have antineoplastic activity in a variety of animal models and human cancer cell lines.

Egyéb megjegyzések

AZD1152-HQPA has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the AZD1152-HPQA probe summary on the Chemical Probes Portal website.

Tárolási osztály kódja

11 - Combustible Solids

WGK

WGK 3

Lobbanási pont (F)

Not applicable

Lobbanási pont (C)

Not applicable


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Analitikai tanúsítványok (COA)

Lot/Batch Number

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Az Ön által nemrégiben megvásárolt termékekre vonatkozó dokumentumokat a Dokumentumtárban találja.

Dokumentumtár megtekintése

Ellen Mitchell et al.
Cell division, 15, 11-11 (2020-09-26)
XMU-MP-1 is an inhibitor of the Hippo pathway kinases MST1/2 and has been shown to promote the downstream activation of the pro-proliferative, pro-regenerative and anti-apoptotic transcriptional regulator YAP1. We tested whether XMU-MP-1 can activate YAP1 in a model human mini-organ
Cell-based screen for altered nuclear phenotypes reveals senescence progression in polyploid cells after Aurora kinase B inhibition
Sadaie M, et al.
Molecular Biology of the Cell, 26(17), 2971-2985 (2015)
Sandhya Noronha et al.
In vitro cellular & developmental biology. Animal, 54(1), 71-84 (2017-12-03)
Liposarcoma is a malignant soft tissue tumor that originates from adipose tissue and is one of the most frequently diagnosed soft tissue sarcomas in humans. There is great interest in identifying novel chemotherapeutic options for treating liposarcoma based upon molecular
Ali Zekri et al.
Journal of molecular neuroscience : MN, 65(4), 444-455 (2018-07-28)
Neuroblastoma (NB) remains the critical challenge in pediatric oncology. It has the highest rate of spontaneous regression among all human cancers. Aurora kinase B (AURKB), a crucial regulator of malignant mitosis, is involved in chromosome segregation and cytokinesis. AZD1152-HQPA (Barasertib)
Human genome-wide RNAi screen reveals host factors required for enterovirus 71 replication
Wu KX, et al.
Nature Communications, 7, 13150-13150 (2016)

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