Barasertib (AZD1152-HQPA)

For research use only. Not for use in humans.

Catalog No.S1147 Synonyms: AZD2811

57 publications

Barasertib (AZD1152-HQPA) 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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Selleck's Barasertib (AZD1152-HQPA) has been 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 MWrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH\5R28xNTVyMDDuUS=> MX20POKhcA>? M4KyNGlEPTB;MkWgcm0> NHTwSHIzPTJ5N{[1PS=>
LNCaP MnnnRZBweHSxc3nzJGF{e2G7 M3HmcVAuPTByIH7N MX[0POKhcA>? NX\QO5hocW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cCC2aILveYdpKGOjc4Dhd4UuOyC3cILl[5Vt[XSrb36= NYXQdVh5OjV{N{e2OVk>
LNCaP NVvLcYJSTnWwY4Tpc44hSXO|YYm= MYe1NEBvVQ>? M3foeVQ5KGh? M3LOTIlv\HWlZYOgcYlkem:wdXPs[Ykhf2m2aDDhcoV2\2WwaXOgcYVkcGGwaYPt NGHKVWYzPTJ5N{[1PS=>
Ramos MX;GeY5kfGmxbjDBd5NigQ>? NFS2eHI2ODBibl2= NHzMZ2MxNTd{IHi= MlL4bY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn MVSyNVM4OTR2Nh?=
Daudi  NHzaRYtHfW6ldHnvckBCe3OjeR?= NHrJ[VI2ODBibl2= NUSxR|c1OC15MjDo NUDtWpA6cW6qaXLpeJMhSXW{b4LhJGIhc2mwYYPl NFrvbpozOTN5MUS0Oi=>
L540 NYKwWlhUTnWwY4Tpc44hSXO|YYm= NIfIZ|E2ODBibl2= NUnvcpZMOC15MjDo NHjVXldqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= MViyNVM4OTR2Nh?=
BJAJ MmfVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV35eHI1PTByIH7N NXjVS4ZYOC15MjDo MXLpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MofvNlE{PzF2NE[=
Ramos MoexS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWW1NFAhdk1? NFH6bnExNTd{IHi= Mne5bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M{LldFIyOzdzNES2
Raji MXTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVe1NFAhdk1? M2T1dVAuPzJiaB?= MWfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NH;VTlAzOTN5MUS0Oi=>
Daudi  MmrDS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnP0OVAxKG6P NIfEXIkxNTd{IHi= NF7HS29qdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NInDZ3czOTN5MUS0Oi=>
L428 MoL0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXq1NFAhdk1? NFzsV|MxNTd{IHi= M2XhbolvcGmkaYTzJINmdGxiZ4Lve5Rp M323flIyOzdzNES2
KM-H2 NIDDdGlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NILXdZM2ODBibl2= NIjCdWYxNTd{IHi= NXjTXXVCcW6qaXLpeJMh[2WubDDndo94fGh? M2jNOVIyOzdzNES2
HDLM-2 M37Le2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{S3bFUxOCCwTR?= MUiwMVczKGh? NGXzVnZqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NFz4e|IzOTN5MUS0Oi=>
L450 NF3ufpJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYW1NFAhdk1? MmW5NE04OiCq NEXWOINqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MYqyNVM4OTR2Nh?=
BJAJ NHTUPW1CeG:ydH;zbZMhSXO|YYm= MnHVOVAxKG6P MUiwMVczKGh? NH3TVJdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MVyyNVM4OTR2Nh?=
Ramos NHLMN2hCeG:ydH;zbZMhSXO|YYm= NXm5NpNbPTByIH7N NYTHPY5FOC15MjDo MX7pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NWHlVHdjOjF|N{G0OFY>
Raji NEHZcIVCeG:ydH;zbZMhSXO|YYm= M37Ob|UxOCCwTR?= M3XMelAuPzJiaB?= MVrpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NXnxfoVSOjF|N{G0OFY>
Daudi  MljzRZBweHSxc3nzJGF{e2G7 NGLPTGI2ODBibl2= NFHDO|MxNTd{IHi= NH7sVodqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NXrINpU3OjF|N{G0OFY>
L428 MmTjRZBweHSxc3nzJGF{e2G7 MVi1NFAhdk1? M1TiN|AuPzJiaB?= M172bolv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NIO0[WQzOTN5MUS0Oi=>
KM-H2 NEjLT4JCeG:ydH;zbZMhSXO|YYm= MV21NFAhdk1? NIDvbYUxNTd{IHi= M3XyPIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M3HZXFIyOzdzNES2
HDLM-2 NXHlNIZ7SXCxcITvd4l{KEG|c3H5 MkfoOVAxKG6P NXW4XJRZOC15MjDo NF7PeG1qdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M{XGelIyOzdzNES2
L450 MUPBdI9xfG:|aYOgRZN{[Xl? M1fzNFUxOCCwTR?= NE[2cIcxNTd{IHi= Ml\nbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NWnze4hLOjF|N{G0OFY>
SW620 NEfNNIlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkjlSWM2OD1zMNMxNk4yKG6P NUf0[5NGOjF{NEWwPVA>
HCT116 MV;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NH[xVoRGSzVyPUGxxtE{NjNibl2= NYPJO4o6OjF{NEWwPVA>
MDA-MB-435 M1ywZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NF3STW8xNTFyMECwJI5O NVXRPGhZOi13IHS= NYLvPFVvTE2VTx?= NUDqT5hNUUN3ME2xNlUhdk1? M3PpOlIxOTd3OUK2
MDA-MB-468 MmqyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2HST|AuOTByMECgcm0> NUjaTIdxOi13IHS= MmnpSG1UVw>? NHzkUlRKSzVyPUG0JI5O MlHVNlAyPzV7Mk[=
MDA-MB-231 NWfQO5hXT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXW3Z3U1OC1zMECwNEBvVQ>? NF\oeW0zNTViZB?= M4[4VmROW09? M3LSe2lEPTB;MUC1JI5O NX71boZHOjBzN{W5NlY>
BT474 NEXoNJlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWmwMVExODByIH7N MXqyMVUh\A>? M4rtdGROW09? MnrkTWM2OD16IH7N NVz6OY5oOjBzN{W5NlY>
MDA-MB-361 NUi4dFRiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT4T2YxNTFyMECwJI5O M3PMT|IuPSCm Mn\ZSG1UVw>? MmewTWM2OD15MDDuUS=> MXKyNFE4PTl{Nh?=
HER18 MmTES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHmzSG0xNTFyMECwJI5O MmOyNk02KGR? NV\zVHV4TE2VTx?= Mnv5TWM2OD1{MDDuUS=> NHPIcm4zODF5NUmyOi=>
HER18 M3f2UGFxd3C2b4Ppd{BCe3OjeR?= Moi2NVAxKG6P NXrnTFRKOC9{ND:0PEBp NHXUWpdFVVOR NHnheYJqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= MXyyNFE4PTl{Nh?=
MDA-MB-231 MlvoRZBweHSxc3nzJGF{e2G7 MoXINVA2KG6P MkT4NE8zPC92ODDo MYDEUXNQ M4nKR4lv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu Ml;INlAyPzV7Mk[=
JHH-1 Mo\5S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MU[wMlPjiJNzMECwxsBvVQ>? MnvOO|IhcA>? MXnFR|UxRTF5LkVCtVEvOCCwTR?= NYDy[HZJOTl7MUO5N|U>
JHH-2 NY\hWWhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXvvT|QyOC5|4pETNVAxOMLibl2= NUi0WVRwPzJiaB?= NGraVnFGSzVyPUKxPE4xyrFzMD64JI5O M17pN|E6QTF|OUO1
JHH-4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHxT4QxNjQkgKOxNFAxyqCwTR?= NFe3R5I4OiCq MWnFR|UxRTF3NT62xtEyPi56IH7N NXLD[ZhQOTl7MUO5N|U>
HuH-1 M{LwNmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWCwMlPjiJNzMECwxsBvVQ>? MkXhO|IhcA>? Ml;HSWM2OD1{Nz6zxtE2NjBibl2= NVnUfpNwOTl7MUO5N|U>
HuH-6 NFPPflhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGnFfFAxNjQkgKOxNFAxyqCwTR?= NHrwPZA4OiCq MXXFR|UxRTNwN9MxNE43KG6P NHjYe4IyQTlzM{mzOS=>
HuH-7 MlXlS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2L5fFAvO+LCk{GwNFDDqG6P NFO1UmI4OiCq M4CzT2VEPTB;Nj64xtExNjNibl2= NUfUZZZpOTl7MUO5N|U>
HLE MojSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Ml7FNE4{6oDVMUCwNOKhdk1? MYC3NkBp NITobYxGSzVyPUS1MlnDuTZwNDDuUS=> MY[xPVkyOzl|NR?=
HLF NIXvenhIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEHZTFAxNjQkgKOxNFAxyqCwTR?= MVS3NkBp NWTTUmd{TUN3ME2xNlYvOcLzMUKuNkBvVQ>? NGS3W2oyQTlzM{mzOS=>
PLC/PRF/5 NFi0eWtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVqwMlPjiJNzMECwxsBvVQ>? NWDne3BHPzJiaB?= M4TtUmVEPTB;N{[uPeKyQS57IH7N MX:xPVkyOzl|NR?=
SK-Hep1 M1L5TWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M37ySVAvO+LCk{GwNFDDqG6P NGTUfII4OiCq NVvvU4pFTUN3ME2yNU46yrFzLkKgcm0> NXzJUVdSOTl7MUO5N|U>
Hep3B M{XPeGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4HnUFAvO+LCk{GwNFDDqG6P NYn6dFNxPzJiaB?= NInTfVZGSzVyPUeuOuKyOS5{IH7N MYSxPVkyOzl|NR?=
HepG2 Mn3QS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NVP2Om5COC5|4pETNVAxOMLibl2= MVK3NkBp MV\FR|UxRTF2LkhCtVEvPyCwTR?= MmHONVk6OTN7M{W=
Ramos M4f4emFxd3C2b4Ppd{BCe3OjeR?= MV:yOU82OC9zMECgcm0> M4e3b|Q5KGh? M{CzR4lv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> M3\1OVE6QDJ|MU[4
Daudi  Mnz6RZBweHSxc3nzJGF{e2G7 MWCyOU82OC9zMECgcm0> NWPjdmhXPDhiaB?= NYG4WFdXcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MYKxPVgzOzF4OB?=
BALM-14 NFjIbGRCeG:ydH;zbZMhSXO|YYm= NYG5em5JOTJwNT:yOU82OCCwTR?= MYq0PEBp NFLDeWdqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> MUWxPVgzOzF4OB?=
BALM-27 NUjPO3NTSXCxcITvd4l{KEG|c3H5 NXj2ToptOTJwNT:yOU82OCCwTR?= MYO0PEBp NVu4W2pOcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M370WlE6QDJ|MU[4
NB4 MWnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M13POFAvODFxMD6xM|Eh|ryP Mn3LOFghcA>? M{Oz[4lvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MlXLNVg{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 AZD2811
Smiles CCN(CCO)CCCOC1=CC=C2C(=NC=NC2=C1)NC3=CC(=N[NH]3)CC(=O)NC4=CC=CC(=C4)F

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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.

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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