Barasertib (AZD1152-HQPA)

Barasertib (AZD1152-HQPA)

Catalog Number:
L002369024APE
Mfr. No.:
APE-A4112
Price:
$233
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      • Overview
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          Background

          Barasertib, previously known as AZD1152-hydroxyquinazoline pyrazol anilide (HQPA), is a potent aurora kinase inhibitor, which is resulted from rapid phosphatase-mediated cleavage of the precursor, AZD1152, in serum following parenteral administration in vivo. It shows inhibitory effects against a broad range of aurora kinases, including aurora A kinase (AKB), aurora B kinase (ABK), and aurora C kinase (ACK) with inhibition constant (Ki) of 1369 nM, 0.36 nM, and 17.0 nM respectively, as well as the FMS-like tyrosine kinase 3 internal tandem duplication (FLT3-ITD) mutation. Barasertib has demonstrated anti-tumor activity against a range tumor cell lines including those of leukaemic acute myeloid leukemia (AML) origin.

      • Properties
        • Alternative Name
          AZD1152-HQPA,AZD-1152HQPA, AZD1152 HPQA,INH 34; 2-[3-[[7-[3-[ethyl(2-hydroxyethyl)amino]propoxy]quinazolin-4-yl]amino]-1H-pyrazol-5-yl]-N-(3-fluorophenyl)acetamide
          CAS Number
          722544-51-6
          Molecular Formula
          C26H30FN7O3
          Molecular Weight
          507.56
          Appearance
          A solid
          Purity
          98.28%
          Solubility
          ≥25.4 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Naheed Arfin Borah, Swatishree Sradhanjali, et al. "Aurora Kinase B Expression, Its Regulation and Therapeutic Targeting in Human Retinoblastoma." Invest Ophthalmol Vis Sci. 2021 Mar 1;62(3):16. PMID:33704359
          2. Maik Schuler, Lindsay Tomlinson, et al. "Experiments in the EpiDerm 3D Skin In Vitro Model and Minipigs In Vivo Indicate Comparatively Lower In Vivo Skin Sensitivity of Topically Applied Aneugenic Compounds." Toxicol Sci. 2021 Feb 26;180(1):103-121. PMID:33481035
          3. Christine M Field, James F Pelletier, et al. "Disassembly of actin and keratin networks by Aurora B kinase at the midplane of cleaving Xenopus laevis eggs." bioRxiv. 2019 January 06.
          4. Shodai Tanaka, Kaori Senda-Murata, et al. "Live cell imaging of anaphase bridge formation and the subsequent cleavage furrow regression induced by the Aurora B kinase inhibitor AZD1152-HQPA." Bioimages. 2017.10.05
          5. Hanley ML, Yoo TY, et al. "Chromosomal passenger complex hydrodynamics suggests chaperoning of the inactive state by nucleoplasmin/nucleophosmin." Mol Biol Cell. 2017 Apr 12. pii: mbc.E16-12-0860. PMID:28404751

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