Barasertib (AZD1152-HQPA)

For research use only.

Catalog No.S1147 Synonyms: AZD2811

65 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 65 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 NIHFOlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NI\5RmcxNTVyMDDuUS=> NYfETFZJPDkEoHi= NXfyT3U1UUN3ME2yOUBvVQ>? NETGVoIzPTJ5N{[1PS=>
LNCaP M{HxVmFxd3C2b4Ppd{BCe3OjeR?= MkPSNE02ODBibl2= MYC0POKhcA>? NFrKPXVqdmS3Y3XzJIFxd3C2b4TpZ{Bk\WyuIHTlZZRpKHSqcn;1[4gh[2G|cHHz[U0{KHWycnXneYxifGmxbh?= MWSyOVI4PzZ3OR?=
LNCaP M4XzfWZ2dmO2aX;uJGF{e2G7 M{ftT|UxKG6P NGT4XFg1QCCq M4rpSYlv\HWlZYOgcYlkem:wdXPs[Ykhf2m2aDDhcoV2\2WwaXOgcYVkcGGwaYPt NYrWVVgxOjV{N{e2OVk>
Ramos NILMdVlHfW6ldHnvckBCe3OjeR?= M4LOS|UxOCCwTR?= NWDMb5VIOC15MjDo NFryeVNqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= M37ER|IyOzdzNES2
Daudi  NVjodXF1TnWwY4Tpc44hSXO|YYm= NWSxbVBiPTByIH7N MU[wMVczKGh? MmrGbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn MYOyNVM4OTR2Nh?=
L540 MXTGeY5kfGmxbjDBd5NigQ>? M2GyeVUxOCCwTR?= NVn3TYJpOC15MjDo MlTLbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn NUDSXFJmOjF|N{G0OFY>
BJAJ NW\zWWpsT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWW1NFAhdk1? MlHqNE04OiCq M1jhUIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M3HPTlIyOzdzNES2
Ramos NELI[pNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXLabpVFPTByIH7N Mn:xNE04OiCq NFe2fFdqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 M1P3e|IyOzdzNES2
Raji NYXqd|d4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MoHSOVAxKG6P M1KydVAuPzJiaB?= MofvbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= MkixNlE{PzF2NE[=
Daudi  MnXPS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWe1NFAhdk1? NH3rSW4xNTd{IHi= NWT6[nNEcW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> M{TvWFIyOzdzNES2
L428 NXrldW5tT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnW2OVAxKG6P MnLmNE04OiCq NH3Od4dqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NW\KfWVrOjF|N{G0OFY>
KM-H2 MmLMS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MkW3OVAxKG6P MljRNE04OiCq MUDpcohq[mm2czDj[YxtKGe{b4f0bC=> NV3F[FExOjF|N{G0OFY>
HDLM-2 Ml;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUe1NFAhdk1? NEX1XoIxNTd{IHi= NFvUcJNqdmirYnn0d{Bk\WyuIHfyc5d1cA>? M{flUlIyOzdzNES2
L450 NV7M[pQ4T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MVi1NFAhdk1? NX64SIt{OC15MjDo NGP3NVlqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MmnsNlE{PzF2NE[=
BJAJ MXXBdI9xfG:|aYOgRZN{[Xl? NFvXfFQ2ODBibl2= MX[wMVczKGh? NWnvWllwcW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NXm5[FNNOjF|N{G0OFY>
Ramos MljaRZBweHSxc3nzJGF{e2G7 Mm[yOVAxKG6P NVnG[XAyOC15MjDo MVvpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M2PjTFIyOzdzNES2
Raji NWnQS5doSXCxcITvd4l{KEG|c3H5 Mmj3OVAxKG6P NEXmdlIxNTd{IHi= NE\rcI5qdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NFr3VpgzOTN5MUS0Oi=>
Daudi  NFXCSnpCeG:ydH;zbZMhSXO|YYm= MXi1NFAhdk1? MViwMVczKGh? NVrsNHY2cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NHzZU2UzOTN5MUS0Oi=>
L428 NU\HS|g4SXCxcITvd4l{KEG|c3H5 NH;DPYM2ODBibl2= NX;RTYRsOC15MjDo MYXpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MlL2NlE{PzF2NE[=
KM-H2 NHjaOWFCeG:ydH;zbZMhSXO|YYm= MmfOOVAxKG6P NWTKTpU1OC15MjDo M4Dqbolv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M{Xkd|IyOzdzNES2
HDLM-2 NGn5XIJCeG:ydH;zbZMhSXO|YYm= MkfiOVAxKG6P MlLVNE04OiCq NH7KWYhqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NWjJS3hUOjF|N{G0OFY>
L450 M2fIbWFxd3C2b4Ppd{BCe3OjeR?= MXy1NFAhdk1? MmD1NE04OiCq Mn7FbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NY[0WnM1OjF|N{G0OFY>
SW620 NYGwV2h6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MmfQSWM2OD1zMNMxNk4yKG6P MYKyNVI1PTB7MB?=
HCT116 Mle3S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MUDFR|UxRTFzwsGzMlMhdk1? M3W1c|IyOjR3MEmw
MDA-MB-435 NX7j[pJNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NGT0[GkxNTFyMECwJI5O M4PkflIuPSCm NHvZc|ZFVVOR NGjiS3pKSzVyPUGyOUBvVQ>? NF3WU24zODF5NUmyOi=>
MDA-MB-468 NYDBS4dGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEH0cWwxNTFyMECwJI5O NF\hR48zNTViZB?= MoX4SG1UVw>? NHWxVHJKSzVyPUG0JI5O MkH6NlAyPzV7Mk[=
MDA-MB-231 NX\pbY97T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXSwMVExODByIH7N MYGyMVUh\A>? NVjERphzTE2VTx?= MnHpTWM2OD1zMEWgcm0> NEjJNFAzODF5NUmyOi=>
BT474 NULLdWlmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEjvfpExNTFyMECwJI5O M4DmTFIuPSCm MlL2SG1UVw>? MkjwTWM2OD16IH7N M2DxZVIxOTd3OUK2
MDA-MB-361 M1T3dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NEDrTXAxNTFyMECwJI5O M{TqPVIuPSCm NEH1WXVFVVOR MXHJR|UxRTdyIH7N NFzTdFAzODF5NUmyOi=>
HER18 NYf4blNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUewMVExODByIH7N MXeyMVUh\A>? M4HxS2ROW09? NUi4WIZXUUN3ME2yNEBvVQ>? M1vWdVIxOTd3OUK2
HER18 NGTHZ5RCeG:ydH;zbZMhSXO|YYm= MoS4NVAxKG6P NXK2PWVCOC9{ND:0PEBp NEXGN2pFVVOR M4HvcIlv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu MXOyNFE4PTl{Nh?=
MDA-MB-231 MYrBdI9xfG:|aYOgRZN{[Xl? NFH4NoIyODVibl2= NIXRSJAxNzJ2L{S4JIg> NH;LR3NFVVOR M1;iSolv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu NV7JTHk2OjBzN{W5NlY>
JHH-1 MkjwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHjGfJExNjQkgKOxNFAxyqCwTR?= NWWyR5pGPzJiaB?= Ml32SWM2OD1zNz60xtEyNjBibl2= NGq2[2kyQTlzM{mzOS=>
JHH-2 NWn0ZVZ[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2OyeVAvO+LCk{GwNFDDqG6P M13CR|czKGh? MnjaSWM2OD1{MUiuNOKyOTBwODDuUS=> NF3uNGQyQTlzM{mzOS=>
JHH-4 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M3LIelAvO+LCk{GwNFDDqG6P MWG3NkBp NEHOTo9GSzVyPUG1OU43yrFzNj64JI5O MU[xPVkyOzl|NR?=
HuH-1 MXvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NI\RT|UxNjQkgKOxNFAxyqCwTR?= NXzEcY5EPzJiaB?= MoDpSWM2OD1{Nz6zxtE2NjBibl2= NGH2fpkyQTlzM{mzOS=>
HuH-6 NEe5dWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGH5T48xNjQkgKOxNFAxyqCwTR?= M1TmOFczKGh? Mo\1SWM2OD1|LkhCtVAvPiCwTR?= NEm0UXoyQTlzM{mzOS=>
HuH-7 NYLX[ooyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnL0NE4{6oDVMUCwNOKhdk1? NXHv[ZI{PzJiaB?= Ml24SWM2OD14LklCtVAvOyCwTR?= MW[xPVkyOzl|NR?=
HLE NYPzWHNmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWCwMlPjiJNzMECwxsBvVQ>? NFqwdYE4OiCq MkfvSWM2OD12NT65xtE3NjRibl2= NHHjZlUyQTlzM{mzOS=>
HLF M3LkV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXewMlPjiJNzMECwxsBvVQ>? M{H1b|czKGh? MUHFR|UxRTF{Nj6xxtEyOi5{IH7N MYWxPVkyOzl|NR?=
PLC/PRF/5 MUfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NYnkelhqOC5|4pETNVAxOMLibl2= MUW3NkBp MUPFR|UxRTd4LkpCtVkvQSCwTR?= M1mxOVE6QTF|OUO1
SK-Hep1 MnnXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MWiwMlPjiJNzMECwxsBvVQ>? NYr6XmdwPzJiaB?= MX\FR|UxRTJzLkpCtVEvOiCwTR?= MVixPVkyOzl|NR?=
Hep3B M3H6Smdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkj3NE4{6oDVMUCwNOKhdk1? M2LDNlczKGh? M4jLPWVEPTB;Nz62xtEyNjJibl2= MkLLNVk6OTN7M{W=
HepG2 MlW1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NIX5NZIxNjQkgKOxNFAxyqCwTR?= NFuyTow4OiCq NFi0[G5GSzVyPUG0MlfDuTFwNzDuUS=> MkLqNVk6OTN7M{W=
Ramos MoDWRZBweHSxc3nzJGF{e2G7 M1nU[FI2NzVyL{GwNEBvVQ>? NX\NTIJXPDhiaB?= NHKz[HdqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> MlvENVk5OjNzNki=
Daudi  NXvKWGk6SXCxcITvd4l{KEG|c3H5 M3f4cVI2NzVyL{GwNEBvVQ>? MXS0PEBp MlHobY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz MYKxPVgzOzF4OB?=
BALM-14 M{nqSmFxd3C2b4Ppd{BCe3OjeR?= M{TXNFEzNjVxMkWvOVAhdk1? MmixOFghcA>? NXPVdIlscW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ NInCSnEyQTh{M{G2PC=>
BALM-27 MWLBdI9xfG:|aYOgRZN{[Xl? MWGxNk42NzJ3L{WwJI5O NGPafHA1QCCq Mkf6bY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz NFz5bmIyQTh{M{G2PC=>
NB4 MlXES5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NYXjN4h4OC5yMT:wMlEwOSEQvF2= MkLjOFghcA>? MkOzbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NYTuTm11OTh|Nke0PFQ>

... 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)

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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