Barasertib (AZD1152-HQPA)

For research use only.

Catalog No.S1147 Synonyms: AZD2811, INH-34

89 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.

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Selleck's Barasertib (AZD1152-HQPA) has been cited by 89 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 NX;KfZRkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MWWwMVUxOCCwTR?= NXPqbmU4PDkEoHi= NYHFW49nUUN3ME2yOUBvVQ>? NFrBN3o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3O|Y2QSd-MkWyO|c3PTl:L3G+
LNCaP MXXBdI9xfG:|aYOgRZN{[Xl? MoPENE02ODBibl2= MXG0POKhcA>? M4Xofolv\HWlZYOgZZBweHSxdHnjJINmdGxiZHXheIghfGi{b4XnbEBk[XOyYYPlMVMhfXC{ZXf1cIF1cW:w NHzScHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3O|Y2QSd-MkWyO|c3PTl:L3G+
LNCaP NG\xWZRHfW6ldHnvckBCe3OjeR?= M1vpTFUxKG6P NEX2bIM1QCCq NF\qVXdqdmS3Y3XzJI1q[3KxboXjcIVqKHerdHigZY5mfWenbnnjJI1m[2ijbnnzcS=> NYXuWXR1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkWyO|c3PTlpPkK1Nlc4PjV7PD;hQi=>
Ramos NXKw[XB7TnWwY4Tpc44hSXO|YYm= NHH3[VA2ODBibl2= MWqwMVczKGh? MVPpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? Mlm1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
Daudi  NH;oU5lHfW6ldHnvckBCe3OjeR?= NVnHdGc2PTByIH7N NV7jcllrOC15MjDo MVzpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? MY[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
L540 MmXlSpVv[3Srb36gRZN{[Xl? MWG1NFAhdk1? M33TRVAuPzJiaB?= MUPpcohq[mm2czDBeZJwemFiQjDrbY5ie2V? NF33eXI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
BJAJ NHX1dHZIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NEmzeoI2ODBibl2= NIDiblExNTd{IHi= MmmxbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M1PadFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Ramos MmjkS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NUXqbJJiPTByIH7N M1L1UlAuPzJiaB?= NF7vdnlqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NIq5W4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Raji MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NFvvR4Q2ODBibl2= MV2wMVczKGh? NFfOfolqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NYHMVmVmRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Daudi  M17VbGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHHNNWw2ODBibl2= MXOwMVczKGh? NHnmc5lqdmirYnn0d{Bk\WyuIHfyc5d1cCC|aXfubYZq[2GwdHz5 NV3K[FFlRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L428 NEm4N|NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MVu1NFAhdk1? NGXNRYMxNTd{IHi= Mmn4bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MoK3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
KM-H2 NULnUHRQT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTpOVAxKG6P M37CWFAuPzJiaB?= MnL0bY5pcWKrdIOgZ4VtdCCpcn;3eIg> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
HDLM-2 MWPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[1NFAhdk1? M3Xxb|AuPzJiaB?= MlfMbY5pcWKrdIOgZ4VtdCCpcn;3eIg> MmLIQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
L450 NXvTPI9LT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MUO1NFAhdk1? M3vCdlAuPzJiaB?= MljObY5pcWKrdIOgZ4VtdCCpcn;3eIg> MnfvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
BJAJ NFG5ZYVCeG:ydH;zbZMhSXO|YYm= NWflSJZ3PTByIH7N M4f1clAuPzJiaB?= MVvpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M33Qb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Ramos Mn;XRZBweHSxc3nzJGF{e2G7 M1XrdVUxOCCwTR?= Ml7BNE04OiCq MknkbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
Raji NHHEfJJCeG:ydH;zbZMhSXO|YYm= MUK1NFAhdk1? MkLHNE04OiCq M4rkXYlv\HWlZYOgZZBweHSxc3nzJIlvKGFidHnt[U1l\XCnbnTlcpQhdWGwbnXy M2ftdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Daudi  M1\uT2Fxd3C2b4Ppd{BCe3OjeR?= MYK1NFAhdk1? NF3WdFMxNTd{IHi= MWnpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NXezRXJPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
L428 M3PR[mFxd3C2b4Ppd{BCe3OjeR?= MVi1NFAhdk1? MV[wMVczKGh? MX7pcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NVu1T|JrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
KM-H2 NH3OSItCeG:ydH;zbZMhSXO|YYm= NHntV3c2ODBibl2= NVfBSVVnOC15MjDo NH;aNVRqdmS3Y3XzJIFxd3C2b4Ppd{BqdiCjIITpcYUu\GWyZX7k[Y51KG2jbn7ldi=> M3zKRVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
HDLM-2 MYrBdI9xfG:|aYOgRZN{[Xl? MlToOVAxKG6P NFjqcHkxNTd{IHi= NWDhSY11cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
L450 NF\1OlRCeG:ydH;zbZMhSXO|YYm= M{jGOVUxOCCwTR?= MYiwMVczKGh? MkL3bY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M4rXRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
SW620 MnfXS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWOwNmx7TUN3ME2xNOKyOi5zIH7N NXjXRWo3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGyOFUxQTBpPkKxNlQ2ODlyPD;hQi=>
HCT116 M{nmW2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NFLMR4FGSzVyPUGxxtE{NjNibl2= M2j4dlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkS1NFkxLz5{MUK0OVA6ODxxYU6=
MDA-MB-435 NU\jdWhST3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= M2\4NVAuOTByMECgcm0> M3XKR|IuPSCm MYPEUXNQ NEH2[JpKSzVyPUGyOUBvVQ>? M1v0UFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUe1PVI3Lz5{MEG3OVkzPjxxYU6=
MDA-MB-468 NXvJXFJyT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MXewMVExODByIH7N MoDKNk02KGR? M1:ydGROW09? M1e3cGlEPTB;MUSgcm0> NWq4cYpLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-231 M4LObWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NHzBenYxNTFyMECwJI5O MUCyMVUh\A>? MkXsSG1UVw>? M4HWUWlEPTB;MUC1JI5O MoLRQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
BT474 MXrHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMVExODByIH7N M3X6ZlIuPSCm MXvEUXNQ MmTCTWM2OD16IH7N MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF5NUmyOkc,OjBzN{W5NlY9N2F-
MDA-MB-361 NEG5XmtIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MYOwMVExODByIH7N NILOSXYzNTViZB?= Mn3DSG1UVw>? M1u3XmlEPTB;N{Cgcm0> MkX3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
HER18 NUG3ZlRqT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NYLDWlFHOC1zMECwNEBvVQ>? NHi2W4kzNTViZB?= MVHEUXNQ MmnRTWM2OD1{MDDuUS=> MknqQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
HER18 NXmxZ4RLSXCxcITvd4l{KEG|c3H5 M4HZU|ExOCCwTR?= MVOwM|I1NzR6IHi= M13SfWROW09? NITJU2lqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= M4Toc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUe1PVI3Lz5{MEG3OVkzPjxxYU6=
MDA-MB-231 MVHBdI9xfG:|aYOgRZN{[Xl? MXyxNFUhdk1? NYTlO3ozOC9{ND:0PEBp MliwSG1UVw>? NHfDXYpqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NX:3OI9vRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
JHH-1 M2n1d2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M{jPbVAvO+LCk{GwNFDDqG6P NH;TWHo4OiCq NFj3NHFGSzVyPUG3MlTDuTFwMDDuUS=> M{fscFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUGzPVM2Lz5zOUmxN|k{PTxxYU6=
JHH-2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIPSeVExNjQkgKOxNFAxyqCwTR?= MnG3O|IhcA>? NIL6VWdGSzVyPUKxPE4xyrFzMD64JI5O NFvNTno9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
JHH-4 Mn7FS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MXOwMlPjiJNzMECwxsBvVQ>? NHrOOok4OiCq MlL6SWM2OD1zNUWuOuKyOTZwODDuUS=> MlPTQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HuH-1 M1XhR2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NUWxWlBKOC5|4pETNVAxOMLibl2= NVPCVZVuPzJiaB?= MXXFR|UxRTJ5LkRCtVUvOCCwTR?= NETD[mQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HuH-6 NY\mRWNiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlTyNE4{6oDVMUCwNOKhdk1? MVS3NkBp MVTFR|UxRTNwN9MxNE43KG6P Mo[2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HuH-7 NGXKb4NIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NGTiWlQxNjQkgKOxNFAxyqCwTR?= NH\od4k4OiCq M4T0UWVEPTB;Nj64xtExNjNibl2= NHfpb|c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HLE NXOzZoVHT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NFu3c48xNjQkgKOxNFAxyqCwTR?= MWm3NkBp NH;hZphGSzVyPUS1MlnDuTZwNDDuUS=> Mnf0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HLF NEnXb2FIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MX:wMlPjiJNzMECwxsBvVQ>? NWPpZ2wxPzJiaB?= NUT4UGxWTUN3ME2xNlYvOcLzMUKuNkBvVQ>? M4PMNlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUGzPVM2Lz5zOUmxN|k{PTxxYU6=
PLC/PRF/5 MnjoS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3e0RVAvO+LCk{GwNFDDqG6P NHHnNmc4OiCq Mn7SSWM2OD15Nj65xtE6Njlibl2= M{jqZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUGzPVM2Lz5zOUmxN|k{PTxxYU6=
SK-Hep1 M{HCOmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NIPFR5AxNjQkgKOxNFAxyqCwTR?= NVHyTmtHPzJiaB?= NGTIUpRGSzVyPUKxMlnDuTFwMjDuUS=> M4DwZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OUGzPVM2Lz5zOUmxN|k{PTxxYU6=
Hep3B NXLTc3M6T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MkjINE4{6oDVMUCwNOKhdk1? NEDYU2I4OiCq M3LFbGVEPTB;Nz62xtEyNjJibl2= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
HepG2 MUPHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MW[wMlPjiJNzMECwxsBvVQ>? M3v4VFczKGh? Mn63SWM2OD1zND63xtEyNjdibl2= NWnQR2dbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUm5NVM6OzVpPkG5PVE{QTN3PD;hQi=>
Ramos NGnZN|RCeG:ydH;zbZMhSXO|YYm= Ml7INlUwPTBxMUCwJI5O MlvLOFghcA>? M12wdolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> M2n3VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
Daudi  MXXBdI9xfG:|aYOgRZN{[Xl? MUWyOU82OC9zMECgcm0> NWXiPI5mPDhiaB?= NFWwVVdqdmO{ZXHz[ZMhfGinIHzleoVteyCxZjD0bIUh[2ynYY\l[EBnd3KvczDv[kBRSVKSIHHu[EBk[XOyYYPlJFM> NH3UV5M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyN|E3QCd-MUm4NlMyPjh:L3G+
BALM-14 NYjkW3FOSXCxcITvd4l{KEG|c3H5 MmjVNVIvPS9{NT:1NEBvVQ>? NY[yPZpuPDhiaB?= M1y5ZYlv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{M{G2PEc,OTl6MkOxOlg9N2F-
BALM-27 MX7BdI9xfG:|aYOgRZN{[Xl? NXH3c2JmOTJwNT:yOU82OCCwTR?= NHfBbmI1QCCq NVTFNWlIcW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ M2L4VlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
NB4 MkHnS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? Mke3NE4xOS9yLkGvNUDPxE1? NEHxWGw1QCCq MWXpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NUSx[3IxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUizOlc1QDRpPkG4N|Y4PDh2PD;hQi=>
HeLa M2HXTWZ2dmO2aX;uJGF{e2G7 M{\wOFEhfU1? MV2yOEBpenN? MUTJcohq[mm2aX;uJI9nKGG3cn;yZUBDKGG3dH;wbI9{eGixconsZZRqd25iaX6gbJVu[W5iSHXMZUBk\WyuczDheEAyKHWPIHHmeIVzKDJ2IHjyd{BjgSCZZYP0[ZJvKGKub4T0bY5o M{PSdFxiKHSjcnfleF0oZ2KuYX7rK{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
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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / 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 MSDS / 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 Active not recruiting Drug: AZD2811|Drug: Azacitidine|Drug: Venetoclax Acute Myeloid Leukaemia AstraZeneca July 31 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.

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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