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 54 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 NW\Cemw5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmTDNE02ODBibl2= NVXPNGl4PDkEoHi= Ml35TWM2OD1{NTDuUS=> NY\HWplrOjV{N{e2OVk>
LNCaP MYXBdI9xfG:|aYOgRZN{[Xl? MVOwMVUxOCCwTR?= Mn3kOFjDqGh? MnnkbY5lfWOnczDhdI9xfG:2aXOgZ4VtdCCmZXH0bEB1cHKxdXfoJINie3Cjc3WtN{B2eHKnZ4XsZZRqd25? Mlz1NlUzPzd4NUm=
LNCaP MV7GeY5kfGmxbjDBd5NigQ>? MV[1NEBvVQ>? M3nYSVQ5KGh? Ml;qbY5lfWOnczDtbYNzd263Y3zlbUB4cXSqIHHu[ZVo\W6rYzDt[YNp[W6rc32= NYDiSVB7OjV{N{e2OVk>
Ramos M1[ydWZ2dmO2aX;uJGF{e2G7 MmTrOVAxKG6P MkLUNE04OiCq MmSzbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn Ml\sNlE{PzF2NE[=
Daudi  NUPhSIx5TnWwY4Tpc44hSXO|YYm= M3PwbFUxOCCwTR?= NI\sfHQxNTd{IHi= M1n4eolvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= Mo\LNlE{PzF2NE[=
L540 MXjGeY5kfGmxbjDBd5NigQ>? MoTmOVAxKG6P MmDTNE04OiCq NIHy[m9qdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= NYHoVZZmOjF|N{G0OFY>
BJAJ NV;SRWVKT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MV61NFAhdk1? Mon1NE04OiCq MnX1bY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NFj6V5EzOTN5MUS0Oi=>
Ramos M324[Gdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIfkepg2ODBibl2= NUPwbYZ6OC15MjDo NIG4XFRqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NYPFeWRmOjF|N{G0OFY>
Raji NEjLSXRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXi1dmZvPTByIH7N M3K5N|AuPzJiaB?= MXPpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MWKyNVM4OTR2Nh?=
Daudi  NILBTIFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NH;odpA2ODBibl2= MlvnNE04OiCq MVfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 MnPENlE{PzF2NE[=
L428 NELQb4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MkX5OVAxKG6P M3jneVAuPzJiaB?= NF;OWo9qdmirYnn0d{Bk\WyuIHfyc5d1cA>? NHPrWHUzOTN5MUS0Oi=>
KM-H2 M1LoV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MYS1NFAhdk1? M{fyR|AuPzJiaB?= Mn7DbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M{f0RVIyOzdzNES2
HDLM-2 NGnmdYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3;oS|UxOCCwTR?= MlT3NE04OiCq MmPIbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NYrDNHg{OjF|N{G0OFY>
L450 MkHRS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmHCOVAxKG6P NITRZ20xNTd{IHi= MojnbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NIHzUYozOTN5MUS0Oi=>
BJAJ M2GxWmFxd3C2b4Ppd{BCe3OjeR?= NH;ZdIo2ODBibl2= NVS0W4o1OC15MjDo MmSwbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MViyNVM4OTR2Nh?=
Ramos MmTiRZBweHSxc3nzJGF{e2G7 M173WFUxOCCwTR?= MU[wMVczKGh? MoLmbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MV:yNVM4OTR2Nh?=
Raji NGLzPVlCeG:ydH;zbZMhSXO|YYm= NH3ydnQ2ODBibl2= MYiwMVczKGh? M4LkV4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MYSyNVM4OTR2Nh?=
Daudi  MkXtRZBweHSxc3nzJGF{e2G7 M{\6UFUxOCCwTR?= M4jWWFAuPzJiaB?= MmjMbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= Mn;sNlE{PzF2NE[=
L428 MWTBdI9xfG:|aYOgRZN{[Xl? MVS1NFAhdk1? Mk\4NE04OiCq MnPLbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M33SeVIyOzdzNES2
KM-H2 NF7jdmhCeG:ydH;zbZMhSXO|YYm= MkDuOVAxKG6P MWWwMVczKGh? MnHIbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MYGyNVM4OTR2Nh?=
HDLM-2 NHTXSHpCeG:ydH;zbZMhSXO|YYm= NFjUe5Y2ODBibl2= MV2wMVczKGh? NV\INoFycW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MYOyNVM4OTR2Nh?=
L450 NEjUeHdCeG:ydH;zbZMhSXO|YYm= MWW1NFAhdk1? NYDmU2k{OC15MjDo M1zCV4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MWmyNVM4OTR2Nh?=
SW620 NUnCR4o{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2X0bWVEPTB;MUFCtVIvOSCwTR?= NGTZV4ozOTJ2NUC5NC=>
HCT116 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4qxV2VEPTB;MUJCtVMvOyCwTR?= M{\iTVIyOjR3MEmw
MDA-MB-435 M4DQUGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEOzWW4xNTFyMECwJI5O MlzmNk02KGR? MUTEUXNQ NFK3VlRKSzVyPUGyOUBvVQ>? NGfERY4zODF5NUmyOi=>
MDA-MB-468 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NV[xSWFvOC1zMECwNEBvVQ>? NFe4NI8zNTViZB?= MmD5SG1UVw>? M{jVUmlEPTB;MUSgcm0> M1XaRVIxOTd3OUK2
MDA-MB-231 NVS5R2dmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIHMbm4xNTFyMECwJI5O NU\hW44yOi13IHS= NGi1VolFVVOR MmjRTWM2OD1zMEWgcm0> NWnObYpNOjBzN{W5NlY>
BT474 NYmzZo1QT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjTNE0yODByMDDuUS=> Mlz4Nk02KGR? MWjEUXNQ MYPJR|UxRThibl2= NYPr[pk3OjBzN{W5NlY>
MDA-MB-361 Ml\VS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1XKdlAuOTByMECgcm0> NGLxPZozNTViZB?= M2rYS2ROW09? MVfJR|UxRTdyIH7N NFfEVJAzODF5NUmyOi=>
HER18 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXwSYd3OC1zMECwNEBvVQ>? MUSyMVUh\A>? MULEUXNQ Ml7PTWM2OD1{MDDuUS=> M2rrVlIxOTd3OUK2
HER18 NEHsSohCeG:ydH;zbZMhSXO|YYm= MlrwNVAxKG6P MXywM|I1NzR6IHi= NXvDfII6TE2VTx?= M4LEcolv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu NFnlVm0zODF5NUmyOi=>
MDA-MB-231 NF7yOnRCeG:ydH;zbZMhSXO|YYm= NV;WcFNvOTB3IH7N MUKwM|I1NzR6IHi= MkHoSG1UVw>? NVzj[2twcW6mdXPld{BieG:ydH;zbZMh[W6mIILl[JVk\XNiY3zvco9o\W6rYzDwc5RmdnSrYXy= NXHYW4F7OjBzN{W5NlY>
JHH-1 M3Thfmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGj5VmMxNjQkgKOxNFAxyqCwTR?= MoDLO|IhcA>? NYmyeGk4TUN3ME2xO{41yrFzLkCgcm0> M1vqOFE6QTF|OUO1
JHH-2 NGXOTmVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVmwMlPjiJNzMECwxsBvVQ>? MmDIO|IhcA>? MW\FR|UxRTJzOD6wxtEyOC56IH7N NUi2bpdDOTl7MUO5N|U>
JHH-4 NYG3eGRYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlXMNE4{6oDVMUCwNOKhdk1? NGjsUVg4OiCq NHfBVXJGSzVyPUG1OU43yrFzNj64JI5O M2joTVE6QTF|OUO1
HuH-1 NEfNcY9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1HHS|AvO+LCk{GwNFDDqG6P MoPrO|IhcA>? NVXHbplSTUN3ME2yO{4{yrF3LkCgcm0> NWPCeVN3OTl7MUO5N|U>
HuH-6 NGLZPVNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MoO1NE4{6oDVMUCwNOKhdk1? NYDBPHNNPzJiaB?= MYrFR|UxRTNwN9MxNE43KG6P MWCxPVkyOzl|NR?=
HuH-7 NHjEVW9Iem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MnzaNE4{6oDVMUCwNOKhdk1? MXK3NkBp NWDoRXA{TUN3ME22MljDuTBwMzDuUS=> MmjtNVk6OTN7M{W=
HLE NGTXeWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MViwMlPjiJNzMECwxsBvVQ>? NUK4fZg6PzJiaB?= MUPFR|UxRTR3LkpCtVYvPCCwTR?= MkjCNVk6OTN7M{W=
HLF M4TCcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUTOR|ZLOC5|4pETNVAxOMLibl2= NVzLbFJzPzJiaB?= MYHFR|UxRTF{Nj6xxtEyOi5{IH7N NIfrT4UyQTlzM{mzOS=>
PLC/PRF/5 MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPHTHAxNjQkgKOxNFAxyqCwTR?= NFnBOHE4OiCq M{LtZ2VEPTB;N{[uPeKyQS57IH7N MXGxPVkyOzl|NR?=
SK-Hep1 NHrmUIVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGfib4gxNjQkgKOxNFAxyqCwTR?= MVO3NkBp MkHuSWM2OD1{MT65xtEyNjJibl2= M4TVeFE6QTF|OUO1
Hep3B NIexXYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NY\SOWk6OC5|4pETNVAxOMLibl2= M4ToW|czKGh? NWPq[nlETUN3ME23MlbDuTFwMjDuUS=> NHLrSIIyQTlzM{mzOS=>
HepG2 NWDQc5duT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1LNZVAvO+LCk{GwNFDDqG6P MmL2O|IhcA>? NXOzcnR{TUN3ME2xOE44yrFzLkegcm0> MWOxPVkyOzl|NR?=
Ramos M2PI[mFxd3C2b4Ppd{BCe3OjeR?= NVzvUpZOOjVxNUCvNVAxKG6P Mom4OFghcA>? M{\uXYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> NV34[m5sOTl6MkOxOlg>
Daudi  M3fKR2Fxd3C2b4Ppd{BCe3OjeR?= Mk\SNlUwPTBxMUCwJI5O MWi0PEBp NVyyfXV2cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MmPNNVk5OjNzNki=
BALM-14 M3PiTmFxd3C2b4Ppd{BCe3OjeR?= NEW1fmsyOi53L{K1M|UxKG6P MWi0PEBp NVnGN4tqcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ NE\zdYgyQTh{M{G2PC=>
BALM-27 NFHzZXJCeG:ydH;zbZMhSXO|YYm= MnP4NVIvPS9{NT:1NEBvVQ>? NWXL[ZpPPDhiaB?= NEDlV2NqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> MV:xPVgzOzF4OB?=
NB4 MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmOyNE4xOS9yLkGvNUDPxE1? NIrxcHE1QCCq MXPpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NE\vT2YyQDN4N{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]
- 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

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