AZD1152-HQPA | Aurora B kinase inhibitor

CAS:
722544-51-6
Catalog Number:
10-4804
Activity:
Aurora B kinase inhibitor
Chemical Name:
3-[[7-[3-[Ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino-N-(3-fluorophenyl)-1H-pyrazole-5-acetamide
Alternate Name:
Barasertib-HQPA; AZD2811
Molecular Weight:
507.56
Molecular Formula:
C26H30FN7O3
Solubility:
Soluble in DMSO (up to 15 mg/ml).
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Available Options

Size:PriceQuantity 
5 mg$50.00
25 mg$150.00

AZD1152-HQPA (722544-51-6) is a potent and highly selective inhibitor of Aurora B.1 Aurora B Ki = 0.36 nM; Aurora A Ki = 1,369 nM.2 It inhibits the growth of tumors in multiple cancer models.3-6 Excessive ROS generation7 and upregulated tumor suppressor miRNAs8 have been proposed as a novel mechanisms of cytotoxicity of AZD1152-HQPA.

References/Citations:

1) Mortlock et al. (2007) Discovery, Synthesis, and in Vivo Activity of a New Class of Pyrazoloquinazolines as Selective Inhibitors of Aurora B Kinase; J. Med. Chem. 50 2213
2) Wilkinson et al. (2007) AZD1152, a Selective Inhibitor of Aurora B Kinase, Inhibits Human Tumor Xenograft Growth by Inducing Apoptosis; Clin. Cancer Res. 13 3682
3) Oke et al. (2009) AZD1152 rapidly and negatively affects the growth and survival of human acute myeloid leukemia cells in vitro and in vivo; Cancer Res. 69 4150
4) Aihara et al. (2010) The selective Aurora B kinase inhibitor AZD1152 as a novel treatment for hepatocellular carcinoma; J. Hepatol. 52 63
5) Mori et al. (2011) Effects of AZD1152, a selective Aurora B kinase inhibitor of Burkitt’s and Hodgkin’s lymphomas; Biochem. Pharmacol. 82 1252
6) Helfrich et al. (2016) Barasertib (AZD1152), a Small Molecule Aurora B Inhibitor, Inhibits the Growth of SCLC Cell Lines In Vitro and In Vivo; Mol. Cancer Ther. 15 2314
7) Zekri et al. (2017) Reactive oxygen species generation and increase in mitochondrial copy number: new insight into the potential mechanism of cytotoxicity induced by aurora kinase inhibitor, AZD1152-HQPA; Anticancer Drugs 28 841
8) Zekri et al. (2018) The Potential Contribution of microRNAs in Anti-cancer Effects of Aurora Kinase Inhibitor (AZD1152-HQPA); J. Mol. Neurosci. 65 444

CAS:
722544-51-6
Catalog Number:
10-4804
Activity:
Aurora B kinase inhibitor
Chemical Name:
3-[[7-[3-[Ethyl(2-hydroxyethyl)amino]propoxy]-4-quinazolinyl]amino-N-(3-fluorophenyl)-1H-pyrazole-5-acetamide
Alternate Name:
Barasertib-HQPA; AZD2811
Molecular Weight:
507.56
Molecular Formula:
C26H30FN7O3
Solubility:
Soluble in DMSO (up to 15 mg/ml).
Physical Properties:
Yellow solid
Purity:
98% by HPLC
NMR (Conforms)
Storage Temperature:
-20°
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee