Barasertib (AZD1152-HQPA)

For research use only.

Catalog No.S1147 Synonyms: AZD2811

71 publications

Barasertib (AZD1152-HQPA) Chemical Structure

CAS No. 722544-51-6

Barasertib (AZD1152-HQPA, AZD2811) 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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Selleck's Barasertib (AZD1152-HQPA) has been cited by 71 publications

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Biological Activity

Description Barasertib (AZD1152-HQPA, AZD2811) 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 NVzuXpBLT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M3zoSlAuPTByIH7N MnzUOFjDqGh? M4TT[WlEPTB;MkWgcm0> MXqyOVI4PzZ3OR?=
LNCaP MWXBdI9xfG:|aYOgRZN{[Xl? MoS2NE02ODBibl2= MWq0POKhcA>? NFHiSnlqdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKHSqcn;1[4gh[2G|cHHz[U0{KHWycnXneYxifGmxbh?= M17vTFI2Ojd5NkW5
LNCaP M2[3NGZ2dmO2aX;uJGF{e2G7 NGnjWIQ2OCCwTR?= MVS0PEBp NV7YNlF2cW6mdXPld{BucWO{b371Z4xmcSC5aYToJIFv\XWpZX7pZ{Bu\WOqYX7pd40> NG[4eHQzPTJ5N{[1PS=>
Ramos NI[4doxHfW6ldHnvckBCe3OjeR?= MXO1NFAhdk1? M3L3XlAuPzJiaB?= MWXpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? MnTBNlE{PzF2NE[=
Daudi  NYC1O2k2TnWwY4Tpc44hSXO|YYm= NFzZWnM2ODBibl2= Mk\WNE04OiCq NXLVZpFIcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl NHPrWIQzOTN5MUS0Oi=>
L540 NI\uUJFHfW6ldHnvckBCe3OjeR?= M1vyOVUxOCCwTR?= NHXxd5YxNTd{IHi= NY\MSZNqcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl MV:yNVM4OTR2Nh?=
BJAJ M37oO2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NELVS5I2ODBibl2= M3Oy[VAuPzJiaB?= NEj2cm5qdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NXLKOnF5OjF|N{G0OFY>
Ramos NHm4NXhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnnd2o2ODBibl2= NFewVlExNTd{IHi= MkPYbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M4G0UlIyOzdzNES2
Raji NEHNUmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYi1NFAhdk1? NEHnW5UxNTd{IHi= MkftbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M2nXelIyOzdzNES2
Daudi  MWTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVHUe3F7PTByIH7N MXGwMVczKGh? Mkf6bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NVzMOWxlOjF|N{G0OFY>
L428 MoXDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2PMXVUxOCCwTR?= NYXvUJhLOC15MjDo MWDpcohq[mm2czDj[YxtKGe{b4f0bC=> MnSyNlE{PzF2NE[=
KM-H2 NHjVWGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HqTVUxOCCwTR?= M1LMclAuPzJiaB?= MoHabY5pcWKrdIOgZ4VtdCCpcn;3eIg> MVKyNVM4OTR2Nh?=
HDLM-2 Mme2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NF\KUYs2ODBibl2= M4LYdVAuPzJiaB?= NUjvTWVOcW6qaXLpeJMh[2WubDDndo94fGh? NUP3fJhROjF|N{G0OFY>
L450 NYXiRVIyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFXT[|k2ODBibl2= NF3B[HgxNTd{IHi= NH\1eXNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? Mn3xNlE{PzF2NE[=
BJAJ MU\BdI9xfG:|aYOgRZN{[Xl? NUX1doxrPTByIH7N NI[4TJkxNTd{IHi= NX3yWoNzcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NUP6TYJwOjF|N{G0OFY>
Ramos MmOwRZBweHSxc3nzJGF{e2G7 MVq1NFAhdk1? MUGwMVczKGh? NHLnUVdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MUOyNVM4OTR2Nh?=
Raji MV\BdI9xfG:|aYOgRZN{[Xl? MkTtOVAxKG6P MnKxNE04OiCq NVvZXJZucW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NGGyc40zOTN5MUS0Oi=>
Daudi  M2\OfWFxd3C2b4Ppd{BCe3OjeR?= MWe1NFAhdk1? NEPoWHgxNTd{IHi= NYTjOndScW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> M{LBV|IyOzdzNES2
L428 MU\BdI9xfG:|aYOgRZN{[Xl? NHvMVJA2ODBibl2= M{\BS|AuPzJiaB?= MlfNbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NV;NcJNpOjF|N{G0OFY>
KM-H2 MXPBdI9xfG:|aYOgRZN{[Xl? M3rFVVUxOCCwTR?= MWiwMVczKGh? M1TIbYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MYOyNVM4OTR2Nh?=
HDLM-2 NGixVGhCeG:ydH;zbZMhSXO|YYm= NHvac3c2ODBibl2= MXSwMVczKGh? NXzEW3F{cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> Mnj6NlE{PzF2NE[=
L450 MoHDRZBweHSxc3nzJGF{e2G7 M2XxUlUxOCCwTR?= NHnEeVMxNTd{IHi= MXTpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NEjsVnkzOTN5MUS0Oi=>
SW620 M{TYOGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NV3jOWU1TUN3ME2xNOKyOi5zIH7N MlTVNlEzPDVyOUC=
HCT116 MmXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYDFR|UxRTFzwsGzMlMhdk1? MXqyNVI1PTB7MB?=
MDA-MB-435 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MX[wMVExODByIH7N M3Pp[FIuPSCm NXTYe|JHTE2VTx?= MYDJR|UxRTF{NTDuUS=> MoTJNlAyPzV7Mk[=
MDA-MB-468 NEjnRlZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MUiwMVExODByIH7N NGG5OoEzNTViZB?= MYjEUXNQ MoLJTWM2OD1zNDDuUS=> MYqyNFE4PTl{Nh?=
MDA-MB-231 NWTvOGpbT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFryfFYxNTFyMECwJI5O M1XZdVIuPSCm MWTEUXNQ M4LOUmlEPTB;MUC1JI5O MWeyNFE4PTl{Nh?=
BT474 MlzNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV:wMVExODByIH7N MXiyMVUh\A>? MmHuSG1UVw>? M2[4SGlEPTB;ODDuUS=> M2DDSVIxOTd3OUK2
MDA-MB-361 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXjFOW1{OC1zMECwNEBvVQ>? MliyNk02KGR? NUL1cJA3TE2VTx?= NXvYPHdbUUN3ME23NEBvVQ>? MoX6NlAyPzV7Mk[=
HER18 MYfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPZeW1FOC1zMECwNEBvVQ>? NUDjNotGOi13IHS= MWrEUXNQ M4fWVWlEPTB;MkCgcm0> MXGyNFE4PTl{Nh?=
HER18 Mn;mRZBweHSxc3nzJGF{e2G7 M2LXfVExOCCwTR?= NF7WTIExNzJ2L{S4JIg> Mn:5SG1UVw>? NF7rUIdqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NEnaUIgzODF5NUmyOi=>
MDA-MB-231 M2[wV2Fxd3C2b4Ppd{BCe3OjeR?= NWmyS3B2OTB3IH7N M4rFclAwOjRxNEigbC=> NEPndYdFVVOR NI[0T4pqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NHvEbVAzODF5NUmyOi=>
JHH-1 Ml7xS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVmwMlPjiJNzMECwxsBvVQ>? NVv4RXFFPzJiaB?= MVTFR|UxRTF5LkVCtVEvOCCwTR?= Mny3NVk6OTN7M{W=
JHH-2 MnH4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVGwMlPjiJNzMECwxsBvVQ>? M4r4dlczKGh? MnTJSWM2OD1{MUiuNOKyOTBwODDuUS=> M2HyTFE6QTF|OUO1
JHH-4 M{HyPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MoDxNE4{6oDVMUCwNOKhdk1? NYfqZ4FXPzJiaB?= NVPUZmVITUN3ME2xOVUvPsLzMU[uPEBvVQ>? MkLQNVk6OTN7M{W=
HuH-1 NXHaNJRVT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvufpR4OC5|4pETNVAxOMLibl2= NIXuXYw4OiCq Mm\kSWM2OD1{Nz6zxtE2NjBibl2= M3XwZVE6QTF|OUO1
HuH-6 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4jYcVAvO+LCk{GwNFDDqG6P NUXsfZlvPzJiaB?= MnTLSWM2OD1|LkhCtVAvPiCwTR?= M2TBclE6QTF|OUO1
HuH-7 NUfWb3RuT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHXmfXgxNjQkgKOxNFAxyqCwTR?= MkLkO|IhcA>? NH7JU|BGSzVyPU[uPOKyOC5|IH7N M3PlSlE6QTF|OUO1
HLE MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M{DESVAvO+LCk{GwNFDDqG6P Ml7HO|IhcA>? MoezSWM2OD12NT65xtE3NjRibl2= NYPuV2RHOTl7MUO5N|U>
HLF MWDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEm5cmgxNjQkgKOxNFAxyqCwTR?= NGqxcGw4OiCq MkPPSWM2OD1zMk[uNeKyOTJwMjDuUS=> M{HHOlE6QTF|OUO1
PLC/PRF/5 M2jjPGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3\4UFAvO+LCk{GwNFDDqG6P M1TuUVczKGh? MmrSSWM2OD15Nj65xtE6Njlibl2= NUj3NHhuOTl7MUO5N|U>
SK-Hep1 MkX1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1TNR|AvO+LCk{GwNFDDqG6P NXjrcVNzPzJiaB?= MVXFR|UxRTJzLkpCtVEvOiCwTR?= Mnf0NVk6OTN7M{W=
Hep3B MnjPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUCwMlPjiJNzMECwxsBvVQ>? NWP1[YU{PzJiaB?= MkPLSWM2OD15LkdCtVEvOiCwTR?= NWj0ZWZ{OTl7MUO5N|U>
HepG2 M4nWOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3S2U|AvO+LCk{GwNFDDqG6P MXq3NkBp MXPFR|UxRTF2LkhCtVEvPyCwTR?= M32zSlE6QTF|OUO1
Ramos MV;BdI9xfG:|aYOgRZN{[Xl? NW[1NpduOjVxNUCvNVAxKG6P NVG2fHdoPDhiaB?= NWWzd3Z{cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MmrHNVk5OjNzNki=
Daudi  NGTx[2tCeG:ydH;zbZMhSXO|YYm= M4PKfVI2NzVyL{GwNEBvVQ>? NXi4Vlg4PDhiaB?= NG\MdFJqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NXfuNZVxOTl6MkOxOlg>
BALM-14 M2WzVmFxd3C2b4Ppd{BCe3OjeR?= MnW3NVIvPS9{NT:1NEBvVQ>? NXn6ZlF2PDhiaB?= MYLpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NYLIN4ZHOTl6MkOxOlg>
BALM-27 M4HlZ2Fxd3C2b4Ppd{BCe3OjeR?= NWP1XmZ1OTJwNT:yOU82OCCwTR?= Mk\nOFghcA>? MnvTbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz NVqxXG9zOTl6MkOxOlg>
NB4 NVLkO3BkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkPxNE4xOS9yLkGvNUDPxE1? NVjiR5BnPDhiaB?= M1vCcIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3HG[VE5OzZ5NEi0

... 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
  • 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)
Water Insoluble
Ethanol '3 mg/mL
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 AZD2811
Smiles CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO

In vivo Formulation Calculator (Clear solution)

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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

Tel: +1-832-582-8158 Ext:3

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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