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 46 Publications

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Choose Selective Aurora Kinase Inhibitors

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 M3zvVGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NYfkXYdMOC13MECgcm0> NYD6UnFPPDkEoHi= MlrsTWM2OD1{NTDuUS=> M4DyeFI2Ojd5NkW5
LNCaP NETvSnBCeG:ydH;zbZMhSXO|YYm= MkfvNE02ODBibl2= NXzTeIFrPDkEoHi= NIDOVVBqdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKHSqcn;1[4gh[2G|cHHz[U0{KHWycnXneYxifGmxbh?= NIDRNGszPTJ5N{[1PS=>
LNCaP NWjLfZQ3TnWwY4Tpc44hSXO|YYm= M324TVUxKG6P NX\JXWVwPDhiaB?= MmXibY5lfWOnczDtbYNzd263Y3zlbUB4cXSqIHHu[ZVo\W6rYzDt[YNp[W6rc32= MmXtNlUzPzd4NUm=
Ramos MXnGeY5kfGmxbjDBd5NigQ>? NWn2XVFTPTByIH7N M1yyT|AuPzJiaB?= NWHOdpJYcW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl MlnqNlE{PzF2NE[=
Daudi  MWXGeY5kfGmxbjDBd5NigQ>? MYi1NFAhdk1? MXmwMVczKGh? M{nNV4lvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= Mlq1NlE{PzF2NE[=
L540 NF3R[JZHfW6ldHnvckBCe3OjeR?= M3S3SVUxOCCwTR?= NXXXd2l[OC15MjDo NUTXemxocW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl NFjVZYEzOTN5MUS0Oi=>
BJAJ M{jjbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M2WyVlUxOCCwTR?= NVPnd2RYOC15MjDo NFTncpNqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NIHK[|czOTN5MUS0Oi=>
Ramos M4faeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1XsOlUxOCCwTR?= M3PDO|AuPzJiaB?= NIKzO2tqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NVrmfoJqOjF|N{G0OFY>
Raji NIPHWpZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NF[3O3c2ODBibl2= M13wfVAuPzJiaB?= NXTScVJQcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MkjyNlE{PzF2NE[=
Daudi  NVPST4VoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlnTOVAxKG6P MVSwMVczKGh? NVfmO4o1cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MYeyNVM4OTR2Nh?=
L428 MlzBS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NU\XW2lLPTByIH7N MlvSNE04OiCq MYfpcohq[mm2czDj[YxtKGe{b4f0bC=> MUCyNVM4OTR2Nh?=
KM-H2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2DZZVUxOCCwTR?= NWrG[VJ{OC15MjDo MVzpcohq[mm2czDj[YxtKGe{b4f0bC=> NXL4WIlEOjF|N{G0OFY>
HDLM-2 M{j6eWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1TRTVUxOCCwTR?= NWLTUHJvOC15MjDo MkXtbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MWCyNVM4OTR2Nh?=
L450 NGT2b41Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1m2NVUxOCCwTR?= MU[wMVczKGh? MmTkbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NWniZYJoOjF|N{G0OFY>
BJAJ MlewRZBweHSxc3nzJGF{e2G7 MkjwOVAxKG6P NYHsV4tsOC15MjDo NFrzXIRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M13zc|IyOzdzNES2
Ramos MmDvRZBweHSxc3nzJGF{e2G7 NX32UFJPPTByIH7N NIq2UpIxNTd{IHi= MXjpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MmfaNlE{PzF2NE[=
Raji NWTlZoJZSXCxcITvd4l{KEG|c3H5 NHjFeGc2ODBibl2= Mli5NE04OiCq NIridmdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NEXQPJQzOTN5MUS0Oi=>
Daudi  MnfuRZBweHSxc3nzJGF{e2G7 MV[1NFAhdk1? NYPlNGJvOC15MjDo NFPJN49qdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NF7jdJkzOTN5MUS0Oi=>
L428 MXHBdI9xfG:|aYOgRZN{[Xl? NH;yboY2ODBibl2= MXywMVczKGh? M1\xRYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NGHaWIEzOTN5MUS0Oi=>
KM-H2 MXHBdI9xfG:|aYOgRZN{[Xl? MmnBOVAxKG6P NV;Zem41OC15MjDo Mmm3bY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MXOyNVM4OTR2Nh?=
HDLM-2 NYTBTZQ2SXCxcITvd4l{KEG|c3H5 MVG1NFAhdk1? MmfYNE04OiCq NVrvUXFIcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MUGyNVM4OTR2Nh?=
L450 MlLyRZBweHSxc3nzJGF{e2G7 MUK1NFAhdk1? MonSNE04OiCq NX;S[5lrcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NYDrUm9YOjF|N{G0OFY>
SW620 NYnYe5l1T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NVvMdFl6TUN3ME2xNOKyOi5zIH7N NV;m[Xp6OjF{NEWwPVA>
HCT116 Mn3yS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MVfFR|UxRTFzwsGzMlMhdk1? NGjw[5IzOTJ2NUC5NC=>
MDA-MB-435 NEnGVotIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYSwMVExODByIH7N NH\lPHkzNTViZB?= NXO1boxbTE2VTx?= Mm\PTWM2OD1zMkWgcm0> NYnIc3FkOjBzN{W5NlY>
MDA-MB-468 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MkjpNE0yODByMDDuUS=> NES4UpUzNTViZB?= M2LWVmROW09? MU\JR|UxRTF2IH7N MUKyNFE4PTl{Nh?=
MDA-MB-231 Ml\CS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1PucVAuOTByMECgcm0> Mlf4Nk02KGR? NYLafmV4TE2VTx?= M3\xVWlEPTB;MUC1JI5O NVLp[JZSOjBzN{W5NlY>
BT474 MWjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV7od2F4OC1zMECwNEBvVQ>? NHX3dFAzNTViZB?= MkHGSG1UVw>? Mn\GTWM2OD16IH7N M13WR|IxOTd3OUK2
MDA-MB-361 NVrqN4VIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M4G2eVAuOTByMECgcm0> M{PVUFIuPSCm NXnRb5NrTE2VTx?= M2q1dmlEPTB;N{Cgcm0> NEH0NnUzODF5NUmyOi=>
HER18 NHvqTGJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFnROIoxNTFyMECwJI5O MljTNk02KGR? MlrYSG1UVw>? NH;LPGJKSzVyPUKwJI5O NV62[|BtOjBzN{W5NlY>
HER18 MkLJRZBweHSxc3nzJGF{e2G7 M{XVV|ExOCCwTR?= NHnHNHgxNzJ2L{S4JIg> MnG5SG1UVw>? MVXpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? MmfkNlAyPzV7Mk[=
MDA-MB-231 NYTybo5VSXCxcITvd4l{KEG|c3H5 NXXQN5Z[OTB3IH7N MV6wM|I1NzR6IHi= NITuU5pFVVOR NHrKS|JqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NXjoSmd7OjBzN{W5NlY>
JHH-1 M4O1SGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUiwMlPjiJNzMECwxsBvVQ>? NUnIbGNkPzJiaB?= NWG5c3FiTUN3ME2xO{41yrFzLkCgcm0> MnLoNVk6OTN7M{W=
JHH-2 NFPLWY1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NVXqdFE4OC5|4pETNVAxOMLibl2= NFPGdHc4OiCq MX;FR|UxRTJzOD6wxtEyOC56IH7N NW\lPItSOTl7MUO5N|U>
JHH-4 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MXiwMlPjiJNzMECwxsBvVQ>? MVy3NkBp NV;pR4JLTUN3ME2xOVUvPsLzMU[uPEBvVQ>? NUi3OJNVOTl7MUO5N|U>
HuH-1 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFH6RmkxNjQkgKOxNFAxyqCwTR?= NEXxfog4OiCq M1fTemVEPTB;MkeuN:KyPS5yIH7N MkjHNVk6OTN7M{W=
HuH-6 NUG3cGg4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NG\FZWgxNjQkgKOxNFAxyqCwTR?= MnLrO|IhcA>? NF7wUpZGSzVyPUOuO:KyOC54IH7N MlTZNVk6OTN7M{W=
HuH-7 NGOxZWFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVSwMlPjiJNzMECwxsBvVQ>? NWXRdJROPzJiaB?= M3XxeGVEPTB;Nj64xtExNjNibl2= M4q3c|E6QTF|OUO1
HLE MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWKxe4JVOC5|4pETNVAxOMLibl2= MmDCO|IhcA>? NEDXcpJGSzVyPUS1MlnDuTZwNDDuUS=> M1fFUlE6QTF|OUO1
HLF MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MonFNE4{6oDVMUCwNOKhdk1? NHPDdpI4OiCq NIfzPI9GSzVyPUGyOk4yyrFzMj6yJI5O MkfjNVk6OTN7M{W=
PLC/PRF/5 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEO3NoExNjQkgKOxNFAxyqCwTR?= MkjHO|IhcA>? NUC0Zml7TUN3ME23Ok46yrF7Lkmgcm0> MmrFNVk6OTN7M{W=
SK-Hep1 MmjaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIXqUo8xNjQkgKOxNFAxyqCwTR?= MnLaO|IhcA>? NYDyVIk6TUN3ME2yNU46yrFzLkKgcm0> MXSxPVkyOzl|NR?=
Hep3B MmjqS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYL3TZN2OC5|4pETNVAxOMLibl2= NHq2UXg4OiCq MXzFR|UxRTdwNtMxNU4zKG6P NXr0T2ZqOTl7MUO5N|U>
HepG2 MlHKS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUWwMlPjiJNzMECwxsBvVQ>? NVjLcXVEPzJiaB?= NIr1N2pGSzVyPUG0MlfDuTFwNzDuUS=> M37ONlE6QTF|OUO1
Ramos MWnBdI9xfG:|aYOgRZN{[Xl? MnnGNlUwPTBxMUCwJI5O M4D5[FQ5KGh? M3fWeolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> MlqyNVk5OjNzNki=
Daudi  M3fmWmFxd3C2b4Ppd{BCe3OjeR?= MoOwNlUwPTBxMUCwJI5O M3\Qc|Q5KGh? MV\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= MnzYNVk5OjNzNki=
BALM-14 M4m0NGFxd3C2b4Ppd{BCe3OjeR?= NGjnfW4yOi53L{K1M|UxKG6P MYe0PEBp NIf2OJBqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NEDUZXAyQTh{M{G2PC=>
BALM-27 MWfBdI9xfG:|aYOgRZN{[Xl? NFz0NogyOi53L{K1M|UxKG6P MoLqOFghcA>? Ml2wbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz MoTtNVk5OjNzNki=
NB4 Ml3DS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmLYNE4xOS9yLkGvNUDPxE1? MmW0OFghcA>? MnP2bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NFLJ[IkyQDN4N{S4OC=>

... 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]
+ Expand
  • 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]
+ Expand
  • 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