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 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 Ml[0S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mn7VNE02ODBibl2= MkXHOFjDqGh? NHfubpFKSzVyPUK1JI5O MkTENlUzPzd4NUm=
LNCaP NFW4UGlCeG:ydH;zbZMhSXO|YYm= MljaNE02ODBibl2= NITUT5M1QMLiaB?= NWjrfXZvcW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cCC2aILveYdpKGOjc4Dhd4UuOyC3cILl[5Vt[XSrb36= M{TaRlI2Ojd5NkW5
LNCaP MnjZSpVv[3Srb36gRZN{[Xl? MV[1NEBvVQ>? NYHaTJhsPDhiaB?= NIX0UHdqdmS3Y3XzJI1q[3KxboXjcIVqKHerdHigZY5mfWenbnnjJI1m[2ijbnnzcS=> M4mzfVI2Ojd5NkW5
Ramos NF;QUoNHfW6ldHnvckBCe3OjeR?= NWL3bFhlPTByIH7N MnnvNE04OiCq NEWwd2ZqdmirYnn0d{BCfXKxcnGgRkBscW6jc3W= MnPXNlE{PzF2NE[=
Daudi  NWfvTJRUTnWwY4Tpc44hSXO|YYm= MUS1NFAhdk1? MlrGNE04OiCq M3:1b4lvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= MWeyNVM4OTR2Nh?=
L540 MYHGeY5kfGmxbjDBd5NigQ>? MkC5OVAxKG6P Mm\1NE04OiCq M3vEbolvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= Mnf2NlE{PzF2NE[=
BJAJ NWLvWGdnT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NH\SdGs2ODBibl2= NXfkV3RQOC15MjDo M3L4TIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= MnnwNlE{PzF2NE[=
Ramos NVXvVFJoT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlvFOVAxKG6P MVywMVczKGh? Mo\WbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NHPFSVAzOTN5MUS0Oi=>
Raji NELxN3pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M2DpblUxOCCwTR?= M4K4R|AuPzJiaB?= MlzybY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NVWyWXJzOjF|N{G0OFY>
Daudi  MlHUS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV;qRow{PTByIH7N M2HFdFAuPzJiaB?= MX;pcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 M4TO[VIyOzdzNES2
L428 NIjtZ4pIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{XN[VUxOCCwTR?= MWWwMVczKGh? NIjTXVhqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NIPCfWgzOTN5MUS0Oi=>
KM-H2 NHHSNlJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NE\wPJA2ODBibl2= MYiwMVczKGh? Mn;HbY5pcWKrdIOgZ4VtdCCpcn;3eIg> NXXKWpVZOjF|N{G0OFY>
HDLM-2 MkTnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MV[1NFAhdk1? NV\3dIVVOC15MjDo M1LwU4lvcGmkaYTzJINmdGxiZ4Lve5Rp MVmyNVM4OTR2Nh?=
L450 MUDHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVSzeYoxPTByIH7N MnjMNE04OiCq M2TCVIlvcGmkaYTzJINmdGxiZ4Lve5Rp MnixNlE{PzF2NE[=
BJAJ MWHBdI9xfG:|aYOgRZN{[Xl? Mn;POVAxKG6P NHTwTJIxNTd{IHi= NFTjNWRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NHnKbFUzOTN5MUS0Oi=>
Ramos M1\5OGFxd3C2b4Ppd{BCe3OjeR?= MWO1NFAhdk1? MnXtNE04OiCq M3\2eIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NH7JdJgzOTN5MUS0Oi=>
Raji NVrGSo1bSXCxcITvd4l{KEG|c3H5 MoK0OVAxKG6P MmLoNE04OiCq NIPjOJFqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NYnNUXZlOjF|N{G0OFY>
Daudi  NX3m[JdzSXCxcITvd4l{KEG|c3H5 NHvIXpE2ODBibl2= MXiwMVczKGh? NIe4WohqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> MmPDNlE{PzF2NE[=
L428 MYLBdI9xfG:|aYOgRZN{[Xl? M3nndFUxOCCwTR?= NHLacmExNTd{IHi= MV\pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MVuyNVM4OTR2Nh?=
KM-H2 MmLWRZBweHSxc3nzJGF{e2G7 MoHNOVAxKG6P NIPMWJIxNTd{IHi= MnvhbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M2DLbVIyOzdzNES2
HDLM-2 MVfBdI9xfG:|aYOgRZN{[Xl? NFTH[Yg2ODBibl2= MmW4NE04OiCq MUnpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M2iwWVIyOzdzNES2
L450 MVzBdI9xfG:|aYOgRZN{[Xl? NX;YU5p4PTByIH7N MY[wMVczKGh? MYHpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NFvCdHAzOTN5MUS0Oi=>
SW620 NFXoSpNIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVPFR|UxRTFywsGyMlEhdk1? NUHsUlNyOjF{NEWwPVA>
HCT116 M1riOWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXPFR|UxRTFzwsGzMlMhdk1? NI\qVpozOTJ2NUC5NC=>
MDA-MB-435 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2wMVExODByIH7N NXziTJJ3Oi13IHS= MUDEUXNQ NILNR5hKSzVyPUGyOUBvVQ>? M33tU|IxOTd3OUK2
MDA-MB-468 MnP4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXKwMVExODByIH7N MojONk02KGR? MXHEUXNQ NE\jWVVKSzVyPUG0JI5O NXv3R|A1OjBzN{W5NlY>
MDA-MB-231 NWD6VGRST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NUm0VolQOC1zMECwNEBvVQ>? NWDWNo1qOi13IHS= MYfEUXNQ NUna[VR5UUN3ME2xNFUhdk1? NYrOTWJtOjBzN{W5NlY>
BT474 M2f4PWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIH3cm4xNTFyMECwJI5O NViyPFl{Oi13IHS= M4O5c2ROW09? MknRTWM2OD16IH7N NEKwc5gzODF5NUmyOi=>
MDA-MB-361 MV\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Ml3sNE0yODByMDDuUS=> M33iZ|IuPSCm MXfEUXNQ NWrLXIFQUUN3ME23NEBvVQ>? MkmyNlAyPzV7Mk[=
HER18 NVTBemVTT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFT0UFIxNTFyMECwJI5O M{K4blIuPSCm MoDUSG1UVw>? NI\sWmxKSzVyPUKwJI5O M1XGU|IxOTd3OUK2
HER18 NXrW[mExSXCxcITvd4l{KEG|c3H5 Mn;qNVAxKG6P NV;LbYhwOC9{ND:0PEBp M2fxWmROW09? MVzpcoR2[2W|IHHwc5B1d3OrczDhcoQhemWmdXPld{BkdG:wb3flcolkKHCxdHXueIlidA>? MonFNlAyPzV7Mk[=
MDA-MB-231 MkC5RZBweHSxc3nzJGF{e2G7 MUGxNFUhdk1? M2\DO|AwOjRxNEigbC=> M2DEOmROW09? Mlf3bY5lfWOnczDhdI9xfG:|aYOgZY5lKHKnZIXj[ZMh[2yxbn;n[Y5q[yCyb4TlcpRq[Wx? Mk\mNlAyPzV7Mk[=
JHH-1 M3;yWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MmixNE4{6oDVMUCwNOKhdk1? NYHwTJc4PzJiaB?= M1HoRmVEPTB;MUeuOOKyOS5yIH7N NHLkUXUyQTlzM{mzOS=>
JHH-2 M3fmcWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn\HNE4{6oDVMUCwNOKhdk1? NEnXXoY4OiCq NELHbVlGSzVyPUKxPE4xyrFzMD64JI5O NIrDUGgyQTlzM{mzOS=>
JHH-4 NX;BV4F[T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnrJNE4{6oDVMUCwNOKhdk1? MV63NkBp Mnr5SWM2OD1zNUWuOuKyOTZwODDuUS=> NEjRfFkyQTlzM{mzOS=>
HuH-1 NF7TVoZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWGwMlPjiJNzMECwxsBvVQ>? NHzn[5c4OiCq MVHFR|UxRTJ5LkRCtVUvOCCwTR?= M4fqOVE6QTF|OUO1
HuH-6 MU\Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVfZPW57OC5|4pETNVAxOMLibl2= MYO3NkBp NWDOe2l6TUN3ME2zMlfDuTBwNjDuUS=> NVyzeYhnOTl7MUO5N|U>
HuH-7 NVz6W2JIT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M1rpTlAvO+LCk{GwNFDDqG6P NIrXZog4OiCq NX\mV2NSTUN3ME22MljDuTBwMzDuUS=> MWOxPVkyOzl|NR?=
HLE MkDIS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV[yRlYxOC5|4pETNVAxOMLibl2= NUjIO|RZPzJiaB?= MV7FR|UxRTR3LkpCtVYvPCCwTR?= M4nZPFE6QTF|OUO1
HLF NYSy[Zo2T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MnjPNE4{6oDVMUCwNOKhdk1? MoXrO|IhcA>? NELjNGlGSzVyPUGyOk4yyrFzMj6yJI5O M{TGRlE6QTF|OUO1
PLC/PRF/5 Mm\4S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlnlNE4{6oDVMUCwNOKhdk1? NXL0WoFvPzJiaB?= M4C4OWVEPTB;N{[uPeKyQS57IH7N NV3EN4s{OTl7MUO5N|U>
SK-Hep1 M{HoUWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MUSwMlPjiJNzMECwxsBvVQ>? MWK3NkBp NEHIdVRGSzVyPUKxMlnDuTFwMjDuUS=> NHHnTYMyQTlzM{mzOS=>
Hep3B M4PBSGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M4m0W|AvO+LCk{GwNFDDqG6P NELBcI44OiCq NGrFe5JGSzVyPUeuOuKyOS5{IH7N MWGxPVkyOzl|NR?=
HepG2 MmXGS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFHF[4MxNjQkgKOxNFAxyqCwTR?= MUG3NkBp MUDFR|UxRTF2LkhCtVEvPyCwTR?= MoTpNVk6OTN7M{W=
Ramos M1LNb2Fxd3C2b4Ppd{BCe3OjeR?= M3fiR|I2NzVyL{GwNEBvVQ>? MonZOFghcA>? NYfyZWtFcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ Mn:xNVk5OjNzNki=
Daudi  NYLpUYJZSXCxcITvd4l{KEG|c3H5 MVSyOU82OC9zMECgcm0> MW[0PEBp MUjpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= Mn7HNVk5OjNzNki=
BALM-14 NUO3fnhiSXCxcITvd4l{KEG|c3H5 MoDLNVIvPS9{NT:1NEBvVQ>? MW[0PEBp MnjGbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz NX3YSmxtOTl6MkOxOlg>
BALM-27 MV3BdI9xfG:|aYOgRZN{[Xl? NVLTUox6OTJwNT:yOU82OCCwTR?= NFTHdYY1QCCq NWewWXN6cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M{HDOVE6QDJ|MU[4
NB4 M4XlV2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NWjufpVjOC5yMT:wMlEwOSEQvF2= NUW0cm5pPDhiaB?= NFvT[ZRqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NG\qWGMyQDN4N{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

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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