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Home > Inhibitors & Agonists > Cell Cycle/DNA Damage > Aurora Kinase

AZD-1152-HPQA

  Cat. No.:  DC1029   Featured
Chemical Structure
722544-51-6
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More than 5000 active chemicals with high quality for research!
Field of application
AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 722544-51-6
Chemical Name: 2-(5-(7-(3-(ethyl(2-hydroxyethyl)amino)propoxy)quinazolin-4-ylamino)-1H-pyrazol-3-yl)-N-(3-fluorophenyl)acetamide
Synonyms: AZD1152-HPQA, AZD-1152-HPQA;AZD 1152-HPQA
SMILES: CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO
Formula: C26H30FN7O3
M.Wt: 507.56
Sotrage: 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
Description: AZD1152-HQPA is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, and appr 3700 fold more selective for Aurora B over Aurora A.
In Vivo: AZD1152 (10-150 mg/kg/day) significantly inhibits the growth of a variety of human solid tumor xenografts, including colon, breast, and lung cancers, in a dose-dependent manner[1]. Administration of AZD1152 (25 mg/kg) alone markedly suppresses the growth of MOLM13 xenografts, confirmed by the observation of necrotic tissue with infiltration of phagocytic cells[2].
In Vitro: AZD1152 displays >3000-fold selectivity for Aurora B as compared with Aurora A which has an IC50 of 1.368 μM. AZD1152 has even less activity against 50 other serine-threonine and tyrosine kinases including FLT3, JAK2, and Abl. AZD1152 inhibits the proliferation of hematopoietic malignant cells such as HL-60, NB4, MOLM13, PALL-1, PALL-2, MV4-11, EOL-1, THP-1, and K562 cells with IC50 of 3-40 nM, displaying appr 100-fold potency than another Aurora kinase inhibitor ZM334739 which has IC50 of 3-30 μM. AZD1152 inhibits the clonogenic growth of MOLM13 and MV4-11 cells with IC50 of 1 nM and 2.8 nM, respectively, as well as the freshly isolated imatinib-resistant leukemia cells with IC50 values of 1-3 nM, more significantly compared with bone marrow mononuclear cells with IC50 values of >10 nM. AZD1152 induces accumulation of cells with 4N/8N DNA content, followed by apoptosis in a dose- and time-dependent manner[2]. AZD1152-HQPA treatment induces defective cell survival, polyploidy, and cell death in LNCaP cell line. AZD1152-HQPA also decreases expression of AR[3].
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC1029 AZD-1152-HPQA AZD1152-HQPA (Barasertib) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM.
DC3106 VX-680 (MK-0457,Tozasertib) VX-680 (MK-0457, Tozasertib) is a pan-Aurora inhibitor of Aurora A, Aurora B and Aurora C with Kiapp of 0.6 nM, 18 nM and 4.6 nM, respectively.
DC2016 MLN8237 (Alisertib) MLN8237 (Alisertib) is a selective Aurora A inhibitor with IC50 of 1.2 nM.
DC1103 Hesperadin Hesperadin inhibits Aurora B and T. brucei Aurora kinase-1 (TbAUK1) with IC50 of 250 nM and 40 nM, respectively.
DC7140 GSK1070916 GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM; displays >100-fold selectivity against the closely related Aurora A-TPX2 complex(IC50=490 nM).
DC7118 ENMD-2076 ENMD-2076 has selective activity against Aurora A and Flt3 with IC50 of 14 nM and 1.86 nM, 25-fold selective for Aurora A than over Aurora B and less potent to VEGFR2/KDR and VEGFR3, FGFR1 and FGFR2 and PDGFRα.
DC7060 AZD1152 AZD1152 (barasertib), pro-drug of barasertib-hQPA, is a selective Aurora B kinase inhibitor, AZD1152 inhibited the proliferation various types of human leukemia cells with an IC50 ranging from 3 nM to 40 nM.
DC7964 Aurora A Inhibitor I Aurora A inhibitor I is a selective Aurora A inhibitor (Aurora A: IC50=0.0034 μM; Aurora B IC50=3.4 μM), (B/A ratio=1000).
DC7070 AT9283 AT9283 is a small molecule a multi-targeted inhibitor with of 4, 1.2, 1.1 and approximate 3 nM for Bcr-Abl(T3151), Jak2 and Jak3, aurora A and B, respectively.
DC9366 AMG 900 AMG 900 is a potent and highly selective pan-Aurora kinases inhibitor for Aurora A/B/C with IC50 of 5 nM/4 nM /1 nM; >10-fold selective for Aurora kinases than p38α, Tyk2, JNK2, Met and Tie2.
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