Barasertib (AZD1152-HQPA,AZD2811)

Catalog No.S1147 Synonyms: INH 34

Barasertib (AZD1152-HQPA,AZD2811) Chemical Structure

Molecular Weight(MW): 507.56

Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.

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Cited by 57 Publications

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Biological Activity

Description Barasertib (AZD1152-HQPA) is a highly selective Aurora B inhibitor with IC50 of 0.37 nM in a cell-free assay, ~3700 fold more selective for Aurora B over Aurora A. Phase 1.
Targets
Aurora B [1]
(Cell-free assay)
0.37 nM
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 ~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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
LNCaP NFLVOWxIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkPCNE02ODBibl2= M4joU|Q5yqCq MofxTWM2OD1{NTDuUS=> MXyyOVI4PzZ3OR?=
LNCaP NGDleYVCeG:ydH;zbZMhSXO|YYm= NX63eFJ{OC13MECgcm0> M3nocFQ5yqCq NWfZd|locW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cCC2aILveYdpKGOjc4Dhd4UuOyC3cILl[5Vt[XSrb36= MYmyOVI4PzZ3OR?=
LNCaP M{XqOWZ2dmO2aX;uJGF{e2G7 NFzGUFE2OCCwTR?= M3HDflQ5KGh? NGCxe|hqdmS3Y3XzJI1q[3KxboXjcIVqKHerdHigZY5mfWenbnnjJI1m[2ijbnnzcS=> MmHuNlUzPzd4NUm=
Ramos NGTlWmZHfW6ldHnvckBCe3OjeR?= NFP5bGg2ODBibl2= MUmwMVczKGh? NXTpT3Z2cW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl MVSyNVM4OTR2Nh?=
Daudi  NVjt[4x7TnWwY4Tpc44hSXO|YYm= MnflOVAxKG6P NUL3ZmljOC15MjDo MWHpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? M2q3c|IyOzdzNES2
L540 NEnYSW1HfW6ldHnvckBCe3OjeR?= M3;GdVUxOCCwTR?= MWGwMVczKGh? M{PseolvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= M{nveFIyOzdzNES2
BJAJ M3X5bGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NXHYO3lkPTByIH7N M2H0bFAuPzJiaB?= NH;vW|BqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M{XRd|IyOzdzNES2
Ramos M1HWfGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYK1NFAhdk1? M1i3[VAuPzJiaB?= NYLVTJRHcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> NFTx[ZIzOTN5MUS0Oi=>
Raji MlTrS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MoXqOVAxKG6P MlLLNE04OiCq NVjVfYg{cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MnHwNlE{PzF2NE[=
Daudi  M4TqVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUi1NFAhdk1? NHLVbFgxNTd{IHi= NXS1epFNcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M1\weVIyOzdzNES2
L428 MlLYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{HYdVUxOCCwTR?= NHP3NHgxNTd{IHi= NXXjOpJpcW6qaXLpeJMh[2WubDDndo94fGh? M2nGN|IyOzdzNES2
KM-H2 M2LPSWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MX[1NFAhdk1? MnPlNE04OiCq MmXlbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2SyeVIyOzdzNES2
HDLM-2 NU[xfWRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVe1e2d1PTByIH7N NG\NWmgxNTd{IHi= NELuboFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? Ml3rNlE{PzF2NE[=
L450 NEPHPXdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnLSYY2ODBibl2= MYKwMVczKGh? NVLWcmVwcW6qaXLpeJMh[2WubDDndo94fGh? NYrk[phIOjF|N{G0OFY>
BJAJ M37kRWFxd3C2b4Ppd{BCe3OjeR?= NEjTUXI2ODBibl2= NV\sbIpTOC15MjDo M1XMfYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NUjPV5F3OjF|N{G0OFY>
Ramos NYLTbphXSXCxcITvd4l{KEG|c3H5 MlznOVAxKG6P NXX6[HlNOC15MjDo NYf5NmV7cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> M33nPVIyOzdzNES2
Raji NXTtc4dqSXCxcITvd4l{KEG|c3H5 NFTaV482ODBibl2= NEPxd|YxNTd{IHi= NXvW[mhbcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NGTWRZczOTN5MUS0Oi=>
Daudi  NXjDWVdUSXCxcITvd4l{KEG|c3H5 MoK2OVAxKG6P MV6wMVczKGh? MYnpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M3LkfVIyOzdzNES2
L428 M2rhc2Fxd3C2b4Ppd{BCe3OjeR?= NHLHPJo2ODBibl2= MlvCNE04OiCq MkPwbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M4\2OVIyOzdzNES2
KM-H2 M1q5OWFxd3C2b4Ppd{BCe3OjeR?= NXLSV29yPTByIH7N MmDZNE04OiCq MXXpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MlnZNlE{PzF2NE[=
HDLM-2 M4fy[WFxd3C2b4Ppd{BCe3OjeR?= NUXXOphwPTByIH7N NY\hN5JiOC15MjDo MmTSbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MWWyNVM4OTR2Nh?=
L450 M{DYcGFxd3C2b4Ppd{BCe3OjeR?= MXm1NFAhdk1? MluwNE04OiCq MnXkbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MYiyNVM4OTR2Nh?=
SW620 NEX4eZlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3rUfmVEPTB;MUFCtVIvOSCwTR?= MmHkNlEzPDVyOUC=
HCT116 MY\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWPFR|UxRTFzwsGzMlMhdk1? MoTWNlEzPDVyOUC=
MDA-MB-435 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MlO4NE0yODByMDDuUS=> MWKyMVUh\A>? NW\wfYk6TE2VTx?= NWLyS45EUUN3ME2xNlUhdk1? MY[yNFE4PTl{Nh?=
MDA-MB-468 NXLVVmZIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYKwMVExODByIH7N MXiyMVUh\A>? Ml3MSG1UVw>? MUDJR|UxRTF2IH7N NIC5XVIzODF5NUmyOi=>
MDA-MB-231 Mn3wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[wMVExODByIH7N NVvp[WEzOi13IHS= M1;Ec2ROW09? MmHyTWM2OD1zMEWgcm0> M1vRcFIxOTd3OUK2
BT474 NYD3RXQ1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmP0NE0yODByMDDuUS=> Ml3DNk02KGR? MX7EUXNQ MlrXTWM2OD16IH7N M375fVIxOTd3OUK2
MDA-MB-361 NYXhSJg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYjRVldPOC1zMECwNEBvVQ>? NIHMPFczNTViZB?= MoTnSG1UVw>? M2XmUGlEPTB;N{Cgcm0> NVS5UIlCOjBzN{W5NlY>
HER18 MnTQS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVrPWHRxOC1zMECwNEBvVQ>? M2rmOlIuPSCm NWrYbm16TE2VTx?= Mn7rTWM2OD1{MDDuUS=> M1zW[lIxOTd3OUK2
HER18 Mn2xRZBweHSxc3nzJGF{e2G7 NFyxPWQyODBibl2= MWewM|I1NzR6IHi= NGDlZmlFVVOR MYjpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? M3PBe|IxOTd3OUK2
MDA-MB-231 M4rUZmFxd3C2b4Ppd{BCe3OjeR?= NX3RPYlbOTB3IH7N NFXW[4cxNzJ2L{S4JIg> MXXEUXNQ MWXpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? MW[yNFE4PTl{Nh?=
JHH-1 NV7ENmllT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFvl[pkxNjQkgKOxNFAxyqCwTR?= NXHJenkyPzJiaB?= NV;zemZmTUN3ME2xO{41yrFzLkCgcm0> M3PCPFE6QTF|OUO1
JHH-2 M2\jb2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmPnNE4{6oDVMUCwNOKhdk1? NXfSVoN1PzJiaB?= MUDFR|UxRTJzOD6wxtEyOC56IH7N M1rzVFE6QTF|OUO1
JHH-4 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3qyfVAvO+LCk{GwNFDDqG6P MmXlO|IhcA>? M2rURWVEPTB;MUW1MlbDuTF4Lkigcm0> MoG2NVk6OTN7M{W=
HuH-1 NFzLcWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmwMlPjiJNzMECwxsBvVQ>? M{L1XFczKGh? Ml3tSWM2OD1{Nz6zxtE2NjBibl2= NFnVN4cyQTlzM{mzOS=>
HuH-6 MljES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnHMNE4{6oDVMUCwNOKhdk1? M{PQTVczKGh? NXXyPINYTUN3ME2zMlfDuTBwNjDuUS=> NWO3U4JOOTl7MUO5N|U>
HuH-7 M4XxXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYKwMlPjiJNzMECwxsBvVQ>? MX63NkBp MWjFR|UxRTZwONMxNE4{KG6P M3;XXlE6QTF|OUO1
HLE NX7mS40{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjjNE4{6oDVMUCwNOKhdk1? NVHVRmZtPzJiaB?= MWXFR|UxRTR3LkpCtVYvPCCwTR?= MmTjNVk6OTN7M{W=
HLF MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFLXXooxNjQkgKOxNFAxyqCwTR?= NXLId4c1PzJiaB?= M1L0UmVEPTB;MUK2MlHDuTF{LkKgcm0> NGOzZm0yQTlzM{mzOS=>
PLC/PRF/5 MUjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUXH[pV1OC5|4pETNVAxOMLibl2= M37NeVczKGh? NIPkdldGSzVyPUe2MlnDuTlwOTDuUS=> NIq5UW8yQTlzM{mzOS=>
SK-Hep1 MnnvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkPnNE4{6oDVMUCwNOKhdk1? MW[3NkBp M4jMU2VEPTB;MkGuPeKyOS5{IH7N NWrUPItiOTl7MUO5N|U>
Hep3B M4ewTmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\WNE4{6oDVMUCwNOKhdk1? MnSxO|IhcA>? MV7FR|UxRTdwNtMxNU4zKG6P MXSxPVkyOzl|NR?=
HepG2 NHLrN5lIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NIf1cYgxNjQkgKOxNFAxyqCwTR?= NWq2fos1PzJiaB?= MlH3SWM2OD1zND63xtEyNjdibl2= MoXQNVk6OTN7M{W=
Ramos M3fMTWFxd3C2b4Ppd{BCe3OjeR?= MVqyOU82OC9zMECgcm0> MYm0PEBp NI\QcGpqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NVP2R|ZlOTl6MkOxOlg>
Daudi  MV7BdI9xfG:|aYOgRZN{[Xl? MVyyOU82OC9zMECgcm0> MlHDOFghcA>? NG\rU4ZqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> MnXGNVk5OjNzNki=
BALM-14 M{joZ2Fxd3C2b4Ppd{BCe3OjeR?= Mk\xNVIvPS9{NT:1NEBvVQ>? M3K5OVQ5KGh? MVrpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= MWKxPVgzOzF4OB?=
BALM-27 NXnX[I9LSXCxcITvd4l{KEG|c3H5 MWGxNk42NzJ3L{WwJI5O Mo\zOFghcA>? NV;Vfmc{cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M1PRXFE6QDJ|MU[4
NB4 NIe5blVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnnGNE4xOS9yLkGvNUDPxE1? NVq5NYhPPDhiaB?= NYPpVW9IcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MkTNNVg{Pjd2OES=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AURKB / pSer10 Histone H3 / TP53 / CDKN1A / MYCN; 

PubMed: 26497213     


Downstream effects of barasertib-induced AURKB inhibition on histone H3 phosphorylation and TP53 protein levels in IMR5 and SK-N-BE (2c) as indicated after 24h (left) and 48h (right). TP53 and its downstream effector CDKN1A were up-regulated by barasertib䲧疝Ỵ疞㧀疜膉痘 瘿⟸෕ᾰƌ෕Ð 㺣痖帉痖Ѐ瑖堘𢡄빢᎒

p53 / p21 / p-p38 / p38 ; 

PubMed: 24782314     


U2OS cells were treated with 50 nm or 100 nm AZD1152 for 24 h. p21, p38, p-p38, and p53 levels were determined by immunoblotting β-actin served as a loading control.

26497213 24782314
Immunofluorescence
p21 ; 

PubMed: 24782314     


U2OS cells were treated as in H. Levels of p21 were analyzed by immunostaining. DNA was counterstained with Hoechst 33258.

24782314
Growth inhibition assay
Cell viability ; 

PubMed: 26497213     


Dose response curves to barasertib at 72h of incubation normalized to the DMSO control sample (mean ± SD, n = 5). The inset depicts the normalized AUCs of each response curve. 

26497213
In vivo 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. [1] In addition, 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. [2]

Protocol

Cell Research:[1]
- Collapse
  • Cell lines: HL-60, NB4, MOLM13, PALL-2, MV4-11, EOL-1, and K562 cells
  • Concentrations: Dissolved in DMSO, final concentrations ~100 nM
  • Incubation Time: 24 or 48 hours
  • Method: Cells are exposed to various concentrations of AZD1152 for 24 or 48 hours. Cell proliferation is measured by 3H-thymidine uptake (isotope added 6 hours before harvest), and the concentration that induced 50% growth inhibition (IC50) is calculated from dose-response curves. Cell cycle analysis is performed by flow cytometry. Cell apoptosis is measured by annexin V–FITC apoptosis detection kit.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Female immune-deficient BALB/c nude mice subcutaneously injected with MOLM13 cells
  • Formulation: Dissolved in 3M Tris, pH 9.0, at a concentration of 2.5 mg/mL
  • Dosages: 5 or 25 mg/kg
  • Administration: Intraperitoneal injection 4 times a week or every another day
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 102 mg/mL (200.96 mM)
Ethanol 3 mg/mL (5.91 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+40% PEG 300+2% Tween 80+ddH2O
For best results, use promptly after mixing.
7mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 507.56
Formula

C26H30FN7O3

CAS No. 722544-51-6
Storage powder
in solvent
Synonyms INH 34

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Frequently Asked Questions

  • Question 1:

    Can you let me know what solvent I can use for Barasertib, cat # S1147, for in vivo use? (IP injection in mice)

  • Answer:

    S1147 Barasertib (AZD1152-HQPA) can be dissolved in 30% PEG400/0.5% Tween80/5% Propylene glycol at 30mg/ml as a clear solution. Usually, when prepare the solution, we will add organic solvents first, then add Tween 80, then water. But this compound can not dissolve in 30% PEG400/0.5% Tween80/5% Propylene glycol clearly. After water was added, it became a clear solution.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID