Barasertib (AZD1152-HQPA)

For research use only.

Catalog No.S1147 Synonyms: AZD2811, INH-34

95 publications

Barasertib (AZD1152-HQPA) Chemical Structure

CAS No. 722544-51-6

Barasertib (AZD1152-HQPA, AZD2811, INH-34) 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.

Selleck's Barasertib (AZD1152-HQPA) has been cited by 95 publications

Purity & Quality Control

Choose Selective Aurora Kinase Inhibitors

Biological Activity

Description Barasertib (AZD1152-HQPA, AZD2811, INH-34) 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 NIjycnZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3XWelAuPTByIH7N Mkf6OFjDqGh? MkLXTWM2OD1{NTDuUS=> M4mwN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mke3OlU6Lz5{NUK3O|Y2QTxxYU6=
LNCaP MV3BdI9xfG:|aYOgRZN{[Xl? MoLCNE02ODBibl2= NGfWUo81QMLiaB?= NWK4c5ZPcW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cCC2aILveYdpKGOjc4Dhd4UuOyC3cILl[5Vt[XSrb36= NH;zVoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3O|Y2QSd-MkWyO|c3PTl:L3G+
LNCaP MUjGeY5kfGmxbjDBd5NigQ>? NESzcXA2OCCwTR?= Mn34OFghcA>? NWjN[3pWcW6mdXPld{BucWO{b371Z4xmcSC5aYToJIFv\XWpZX7pZ{Bu\WOqYX7pd40> Mo[0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjV{N{e2OVkoRjJ3Mke3OlU6RC:jPh?=
Ramos M4L1cWZ2dmO2aX;uJGF{e2G7 M{HwXVUxOCCwTR?= NF6xTmYxNTd{IHi= MVvpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? MkTjQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
Daudi  NYfwbIkzTnWwY4Tpc44hSXO|YYm= MVm1NFAhdk1? NHPI[nAxNTd{IHi= M3\4ZolvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= NV65Tmt[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L540 M120bmZ2dmO2aX;uJGF{e2G7 NX;ZW25vPTByIH7N MUCwMVczKGh? M1nieIlvcGmkaYTzJGF2em:{YTDCJItqdmG|ZR?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
BJAJ NGPBXXJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M4DMTlUxOCCwTR?= M33WOFAuPzJiaB?= MkHibY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= NG[2N449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Ramos MlPYS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NEPzUVc2ODBibl2= MoLVNE04OiCq NFfweIdqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
Raji NVy1dlRJT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NIT1SIM2ODBibl2= MVWwMVczKGh? NXXwdII4cW6qaXLpeJMh[2WubDDndo94fGhic3nncolncWOjboTsfS=> Ml3iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
Daudi  M2TsXGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NITKTWI2ODBibl2= M2r4RVAuPzJiaB?= M16yfIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NWL5cYMyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L428 NEDjd|FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M1exe|UxOCCwTR?= NF3ZWYQxNTd{IHi= MoH6bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmC2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
KM-H2 NITCZmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXTxfYZzPTByIH7N MYmwMVczKGh? NGHVVFFqdmirYnn0d{Bk\WyuIHfyc5d1cA>? NYjQO3V{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
HDLM-2 MYrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MknKOVAxKG6P M17VXVAuPzJiaB?= M37NSolvcGmkaYTzJINmdGxiZ4Lve5Rp NV7BXVVORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L450 NUfvNmhGT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFjhUZY2ODBibl2= Mlr0NE04OiCq MkXqbY5pcWKrdIOgZ4VtdCCpcn;3eIg> M{fzW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
BJAJ M1:5PWFxd3C2b4Ppd{BCe3OjeR?= MnjUOVAxKG6P MXKwMVczKGh? MUPpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NXTzPYVURGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Ramos MY\BdI9xfG:|aYOgRZN{[Xl? MV[1NFAhdk1? MVuwMVczKGh? NH;NXFdqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> NInuWJQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Raji MnjYRZBweHSxc3nzJGF{e2G7 MV61NFAhdk1? MUewMVczKGh? M12zbIlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy MV:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
Daudi  NWT6S4RTSXCxcITvd4l{KEG|c3H5 MWq1NFAhdk1? NYXpRWZLOC15MjDo MkG2bY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NGDxUZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
L428 MWfBdI9xfG:|aYOgRZN{[Xl? MoPaOVAxKG6P MXiwMVczKGh? M4Ptc4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NEXpe4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
KM-H2 M4qyOmFxd3C2b4Ppd{BCe3OjeR?= MmfROVAxKG6P NFXrbpAxNTd{IHi= MVTpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NXv2R4RmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
HDLM-2 M3XVZmFxd3C2b4Ppd{BCe3OjeR?= NVXEd4hrPTByIH7N NGLoXJUxNTd{IHi= M1vPc4lv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy NFrySGY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
L450 NILNdG1CeG:ydH;zbZMhSXO|YYm= M3TvdFUxOCCwTR?= MXqwMVczKGh? MXHpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MUC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
SW620 MVjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M4eyVmVEPTB;MUFCtVIvOSCwTR?= NEnUOGM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUK0OVA6OCd-MkGyOFUxQTB:L3G+
HCT116 M{j1Zmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUDrSIpNTUN3ME2xNeKyOy5|IH7N NXfvOJk{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyOFUxQTBpPkKxNlQ2ODlyPD;hQi=>
MDA-MB-435 M{XWVWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXWwMVExODByIH7N MWCyMVUh\A>? Mo\oSG1UVw>? NXvnR5AxUUN3ME2xNlUhdk1? NUGzXHF5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-468 NI\aWWZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3uxT|AuOTByMECgcm0> NFLt[oIzNTViZB?= NYTkXFloTE2VTx?= NXWy[5lZUUN3ME2xOEBvVQ>? NXvqelRzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-231 MWLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M2LFT|AuOTByMECgcm0> MUmyMVUh\A>? Mn30SG1UVw>? MWDJR|UxRTFyNTDuUS=> NE\Lc209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG3OVkzPid-MkCxO|U6OjZ:L3G+
BT474 Ml71S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXPU5dsOC1zMECwNEBvVQ>? NF32doUzNTViZB?= MVfEUXNQ M1zvc2lEPTB;ODDuUS=> Mo\XQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
MDA-MB-361 NE\DbWRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M{P6SlAuOTByMECgcm0> M3OyfFIuPSCm NW\ENIJmTE2VTx?= Ml65TWM2OD15MDDuUS=> NW\aOIV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
HER18 NXv0THdNT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M{flSFAuOTByMECgcm0> M3W1blIuPSCm MYjEUXNQ NF63eoRKSzVyPUKwJI5O NInJRWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG3OVkzPid-MkCxO|U6OjZ:L3G+
HER18 M2jJZWFxd3C2b4Ppd{BCe3OjeR?= MWexNFAhdk1? NXXMVXhzOC9{ND:0PEBp M2rPXGROW09? M3H4dIlv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu NX;6cotXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-231 MWPBdI9xfG:|aYOgRZN{[Xl? NIe4UXIyODVibl2= MXGwM|I1NzR6IHi= MWfEUXNQ NUjqWnpKcW6mdXPld{BieG:ydH;zbZMh[W6mIILl[JVk\XNiY3zvco9o\W6rYzDwc5RmdnSrYXy= NYni[Y5xRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
JHH-1 M{jT[2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mkn2NE4{6oDVMUCwNOKhdk1? NWnmSIk6PzJiaB?= NG[4[YNGSzVyPUG3MlTDuTFwMDDuUS=> NVnEeFdqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
JHH-2 M3zqWGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M3zJNlAvO+LCk{GwNFDDqG6P NIXoSYY4OiCq MUDFR|UxRTJzOD6wxtEyOC56IH7N MljhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
JHH-4 MlzvS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1qxZlAvO+LCk{GwNFDDqG6P MlvBO|IhcA>? NVzUNY5uTUN3ME2xOVUvPsLzMU[uPEBvVQ>? NV;X[5B6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HuH-1 NXvJSYM5T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2rhZ|AvO+LCk{GwNFDDqG6P NHPUSXI4OiCq MnrwSWM2OD1{Nz6zxtE2NjBibl2= MX:8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
HuH-6 MXXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NEDB[W4xNjQkgKOxNFAxyqCwTR?= Ml73O|IhcA>? MV;FR|UxRTNwN9MxNE43KG6P Mo\DQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HuH-7 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NHL2PFAxNjQkgKOxNFAxyqCwTR?= NUXhUXA1PzJiaB?= NV\DXGxJTUN3ME22MljDuTBwMzDuUS=> NE\RcpY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HLE MUTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVXIWJNqOC5|4pETNVAxOMLibl2= NELub4Y4OiCq NXzyfpdJTUN3ME20OU46yrF4LkSgcm0> NWfHR4tiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
HLF NFHlfmdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NFroXXUxNjQkgKOxNFAxyqCwTR?= NXPjfpBFPzJiaB?= M2jMV2VEPTB;MUK2MlHDuTF{LkKgcm0> M1L3XFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUGzPVM2Lz5zOUmxN|k{PTxxYU6=
PLC/PRF/5 Mn;GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MlvKNE4{6oDVMUCwNOKhdk1? NGDwZWg4OiCq MkXHSWM2OD15Nj65xtE6Njlibl2= NI\JRWM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
SK-Hep1 MYjHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MUiwMlPjiJNzMECwxsBvVQ>? MkHuO|IhcA>? MnfpSWM2OD1{MT65xtEyNjJibl2= MYS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
Hep3B NIHMfJdIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MXOwMlPjiJNzMECwxsBvVQ>? Mn:5O|IhcA>? M3uxNGVEPTB;Nz62xtEyNjJibl2= MmnZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HepG2 NXSwVmtRT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFuyZXExNjQkgKOxNFAxyqCwTR?= M{i5elczKGh? NEO2PJlGSzVyPUG0MlfDuTFwNzDuUS=> MmLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
Ramos NFPUXI9CeG:ydH;zbZMhSXO|YYm= MWGyOU82OC9zMECgcm0> M{O3bVQ5KGh? MUnpcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NILxd5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyN|E3QCd-MUm4NlMyPjh:L3G+
Daudi  NFvrPIxCeG:ydH;zbZMhSXO|YYm= MojYNlUwPTBxMUCwJI5O NUTwSYVbPDhiaB?= MV\pcoNz\WG|ZYOgeIhmKGyndnXsd{Bw\iC2aHWgZ4xm[X[nZDDmc5JueyCxZjDQRXJRKGGwZDDjZZNx[XOnIEO= NV21eWZGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4NlMyPjhpPkG5PFI{OTZ6PD;hQi=>
BALM-14 M{P5OmFxd3C2b4Ppd{BCe3OjeR?= NInwWGgyOi53L{K1M|UxKG6P NXTOb2poPDhiaB?= NHr2U4ZqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> M3fJ[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
BALM-27 NYHzfJdpSXCxcITvd4l{KEG|c3H5 NY[1S3BMOTJwNT:yOU82OCCwTR?= MXq0PEBp M4P1OYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> NXLxe|JkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm4NlMyPjhpPkG5PFI{OTZ6PD;hQi=>
NB4 NX\lPGNzT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M17EdVAvODFxMD6xM|Eh|ryP NFzvd201QCCq MVfpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NUP1OZpSRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOlc1QDRpPkG4N|Y4PDh2PD;hQi=>
HeLa NIXCXFNHfW6ldHnvckBCe3OjeR?= MXOxJJVO MoDTNlQhcHK| MV\Jcohq[mm2aX;uJI9nKGG3cn;yZUBDKGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iSHXMZUBk\WyuczDheEAyKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5o M{fiSFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyNki0OVQ6Lz5{ME[4OFU1QTxxYU6=

... 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]
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  • 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)
Water Insoluble
Ethanol '3 mg/mL
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, INH-34
Smiles CCN(CCCOC1=CC2=C(C=C1)C(=NC=N2)NC3=NNC(=C3)CC(=O)NC4=CC(=CC=C4)F)CCO

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 ()
% DMSO % % Tween 80 % ddH2O
CalculateReset

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (mg) = Concentration (mM) × Volume (mL) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and SDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and SDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03217838 Terminated Drug: AZD2811|Drug: Azacitidine|Drug: Venetoclax Acute Myeloid Leukaemia AstraZeneca November 27 2017 Phase 1|Phase 2
NCT02579226 Completed Drug: AZD2811 Advanced Solid Tumours AstraZeneca October 28 2015 Phase 1

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.

  • * Indicates a Required Field

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