Barasertib (AZD1152-HQPA)

For research use only.

Catalog No.S1147 Synonyms: AZD2811

66 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 66 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 M3zRVmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEXlZ|UxNTVyMDDuUS=> MVi0POKhcA>? NELhdZVKSzVyPUK1JI5O M4CxSFI2Ojd5NkW5
LNCaP M{\rOWFxd3C2b4Ppd{BCe3OjeR?= NFfmbGsxNTVyMDDuUS=> NUnLSphHPDkEoHi= NVHPOY5McW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cCC2aILveYdpKGOjc4Dhd4UuOyC3cILl[5Vt[XSrb36= M{fBWFI2Ojd5NkW5
LNCaP MVTGeY5kfGmxbjDBd5NigQ>? NIXDe2U2OCCwTR?= M4LQblQ5KGh? NHqxfYpqdmS3Y3XzJI1q[3KxboXjcIVqKHerdHigZY5mfWenbnnjJI1m[2ijbnnzcS=> NXTETHUyOjV{N{e2OVk>
Ramos Mo[2SpVv[3Srb36gRZN{[Xl? MkHEOVAxKG6P MkXrNE04OiCq M1nX[YlvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= MVOyNVM4OTR2Nh?=
Daudi  MX\GeY5kfGmxbjDBd5NigQ>? NX3UfZMxPTByIH7N M4CzT|AuPzJiaB?= MkDkbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn M1jidlIyOzdzNES2
L540 M4radmZ2dmO2aX;uJGF{e2G7 Mn;4OVAxKG6P NU\sdo5LOC15MjDo NGTZcFZqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= MUCyNVM4OTR2Nh?=
BJAJ MULHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NULheJB5PTByIH7N MUSwMVczKGh? NFLiR3JqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MmPQNlE{PzF2NE[=
Ramos MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHzQfYw2ODBibl2= MkPXNE04OiCq NUH0cHV[cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> MXeyNVM4OTR2Nh?=
Raji MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUm1NFAhdk1? NIXyZ2cxNTd{IHi= MmC2bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MnPUNlE{PzF2NE[=
Daudi  NUnqb4huT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2mzVlUxOCCwTR?= MYiwMVczKGh? MkfPbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MUSyNVM4OTR2Nh?=
L428 NVjsepJGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NWP1[VhYPTByIH7N MXuwMVczKGh? M3zJcIlvcGmkaYTzJINmdGxiZ4Lve5Rp NVro[|BnOjF|N{G0OFY>
KM-H2 NIntTGFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NWTBeWlPPTByIH7N NEjjWVkxNTd{IHi= NX3NO49LcW6qaXLpeJMh[2WubDDndo94fGh? MVOyNVM4OTR2Nh?=
HDLM-2 MmTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MnLCOVAxKG6P MYCwMVczKGh? MoTvbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M2i4ZVIyOzdzNES2
L450 Mnn2S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M2i3S|UxOCCwTR?= Mof2NE04OiCq MV\pcohq[mm2czDj[YxtKGe{b4f0bC=> NXzKbFN7OjF|N{G0OFY>
BJAJ MVTBdI9xfG:|aYOgRZN{[Xl? MUK1NFAhdk1? M{j5eVAuPzJiaB?= MWHpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NXy3bIRxOjF|N{G0OFY>
Ramos NVLDS|VSSXCxcITvd4l{KEG|c3H5 NWPOS4RqPTByIH7N MlrhNE04OiCq MULpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MWmyNVM4OTR2Nh?=
Raji MWnBdI9xfG:|aYOgRZN{[Xl? NXvOUZRQPTByIH7N MnHyNE04OiCq M{H3TIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NXG1dFhPOjF|N{G0OFY>
Daudi  NYH3dlU2SXCxcITvd4l{KEG|c3H5 NVvXZm1EPTByIH7N NHXjdI4xNTd{IHi= MV3pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MX2yNVM4OTR2Nh?=
L428 NXm0XVVJSXCxcITvd4l{KEG|c3H5 NHr0Wmk2ODBibl2= MnXSNE04OiCq NUX2RnI3cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NVzR[ItJOjF|N{G0OFY>
KM-H2 NVvOPXp[SXCxcITvd4l{KEG|c3H5 MnPVOVAxKG6P M1[2PFAuPzJiaB?= M3G1O4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M4XFPVIyOzdzNES2
HDLM-2 M1rNWmFxd3C2b4Ppd{BCe3OjeR?= MWO1NFAhdk1? MXOwMVczKGh? M13NSYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MXWyNVM4OTR2Nh?=
L450 MlfKRZBweHSxc3nzJGF{e2G7 NECwTGk2ODBibl2= MWmwMVczKGh? M4HJPYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M2riXVIyOzdzNES2
SW620 Ml3uS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXjFR|UxRTFywsGyMlEhdk1? NWrHSZdFOjF{NEWwPVA>
HCT116 MWXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYfFR|UxRTFzwsGzMlMhdk1? NF7UXHIzOTJ2NUC5NC=>
MDA-MB-435 NUnteo1YT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MorZNE0yODByMDDuUS=> M1zHdlIuPSCm M3fTVWROW09? NHT0WINKSzVyPUGyOUBvVQ>? NYLp[XI1OjBzN{W5NlY>
MDA-MB-468 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NF61NWsxNTFyMECwJI5O NHjEd4YzNTViZB?= MoP6SG1UVw>? M3exPWlEPTB;MUSgcm0> MorRNlAyPzV7Mk[=
MDA-MB-231 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MViwMVExODByIH7N M{jPblIuPSCm MnmxSG1UVw>? NG\YflBKSzVyPUGwOUBvVQ>? MmDNNlAyPzV7Mk[=
BT474 MlTkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M{fRV|AuOTByMECgcm0> MYKyMVUh\A>? NUnOcndSTE2VTx?= MULJR|UxRThibl2= MVGyNFE4PTl{Nh?=
MDA-MB-361 MoDVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIGzUHoxNTFyMECwJI5O NG[0dHIzNTViZB?= MXvEUXNQ NV\PZYRwUUN3ME23NEBvVQ>? NHzORZAzODF5NUmyOi=>
HER18 MoKyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWewUYszOC1zMECwNEBvVQ>? Mm[5Nk02KGR? NY\ENHJ2TE2VTx?= MU\JR|UxRTJyIH7N NXPBTFBlOjBzN{W5NlY>
HER18 MWXBdI9xfG:|aYOgRZN{[Xl? MY[xNFAhdk1? NGn2b2IxNzJ2L{S4JIg> NWDn[4lJTE2VTx?= NFThdZhqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= MVuyNFE4PTl{Nh?=
MDA-MB-231 NETW[41CeG:ydH;zbZMhSXO|YYm= M2PHNlExPSCwTR?= NWLFUmR{OC9{ND:0PEBp M1jrTGROW09? Mke2bY5lfWOnczDhdI9xfG:|aYOgZY5lKHKnZIXj[ZMh[2yxbn;n[Y5q[yCyb4TlcpRq[Wx? NXj6TIkyOjBzN{W5NlY>
JHH-1 MmX0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKwMlPjiJNzMECwxsBvVQ>? NXfNU3J7PzJiaB?= NFTxe4FGSzVyPUG3MlTDuTFwMDDuUS=> M{DDZlE6QTF|OUO1
JHH-2 NUSzPXFkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTXNE4{6oDVMUCwNOKhdk1? NUS5cJBwPzJiaB?= MV7FR|UxRTJzOD6wxtEyOC56IH7N MnrBNVk6OTN7M{W=
JHH-4 MnvNS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHDNE4{6oDVMUCwNOKhdk1? M1vWblczKGh? NWHzc|MyTUN3ME2xOVUvPsLzMU[uPEBvVQ>? MU[xPVkyOzl|NR?=
HuH-1 NILQOZdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEW3RoQxNjQkgKOxNFAxyqCwTR?= NX3KUm9lPzJiaB?= MVfFR|UxRTJ5LkRCtVUvOCCwTR?= NH7MWI0yQTlzM{mzOS=>
HuH-6 MmXwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXqwMlPjiJNzMECwxsBvVQ>? NWXzWnpSPzJiaB?= MYTFR|UxRTNwN9MxNE43KG6P NVy5fo1xOTl7MUO5N|U>
HuH-7 NXza[WxGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmPNNE4{6oDVMUCwNOKhdk1? Ml30O|IhcA>? MlXCSWM2OD14LklCtVAvOyCwTR?= MoO3NVk6OTN7M{W=
HLE NWPpNIROT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MYmwMlPjiJNzMECwxsBvVQ>? MnT1O|IhcA>? NFTYSpVGSzVyPUS1MlnDuTZwNDDuUS=> NVHWPGszOTl7MUO5N|U>
HLF NX33OmhsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWSwMlPjiJNzMECwxsBvVQ>? M1zySFczKGh? MVHFR|UxRTF{Nj6xxtEyOi5{IH7N NFvV[IEyQTlzM{mzOS=>
PLC/PRF/5 NHK0Z5pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mlf3NE4{6oDVMUCwNOKhdk1? M2S0flczKGh? NHnobnlGSzVyPUe2MlnDuTlwOTDuUS=> MV:xPVkyOzl|NR?=
SK-Hep1 NFiwTo1Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2iyO|AvO+LCk{GwNFDDqG6P MmXBO|IhcA>? NX3Vd2hwTUN3ME2yNU46yrFzLkKgcm0> NXnSfnNCOTl7MUO5N|U>
Hep3B MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzyXFZtOC5|4pETNVAxOMLibl2= MX23NkBp NVX5e5ZiTUN3ME23MlbDuTFwMjDuUS=> NH7zOYsyQTlzM{mzOS=>
HepG2 M3vPfWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWTzTZNXOC5|4pETNVAxOMLibl2= NV;weYhCPzJiaB?= NGLqfZpGSzVyPUG0MlfDuTFwNzDuUS=> NVmxPFN6OTl7MUO5N|U>
Ramos M3\tTmFxd3C2b4Ppd{BCe3OjeR?= NFy0RVgzPS93MD:xNFAhdk1? M3;QflQ5KGh? NFPjelRqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> MUOxPVgzOzF4OB?=
Daudi  MY\BdI9xfG:|aYOgRZN{[Xl? MX2yOU82OC9zMECgcm0> MVe0PEBp NHrLfWRqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> M2rNPVE6QDJ|MU[4
BALM-14 MlnKRZBweHSxc3nzJGF{e2G7 NXHNT|AyOTJwNT:yOU82OCCwTR?= NEjZTFI1QCCq Mm\1bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz M1[3XFE6QDJ|MU[4
BALM-27 NGTLOnFCeG:ydH;zbZMhSXO|YYm= NXO2bJBTOTJwNT:yOU82OCCwTR?= NF;WNIY1QCCq NYL4PY9ocW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M3Lrd|E6QDJ|MU[4
NB4 MXnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWDaRYw6OC5yMT:wMlEwOSEQvF2= MXO0PEBp M{nzOolvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MVKxPFM3PzR6NB?=

... 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)
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

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Dosage mg/kg Average weight of animals g Dosing volume per animal ul Number of animals
Step 2: Enter the in vivo formulation (Different batches have different solubility ratios, please contact Selleck to provide you with the correct ratio)
% DMSO % % Tween 80 % ddH2O
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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

If you have any other enquiries, please leave a message.

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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