Barasertib (AZD1152-HQPA)

For research use only.

Catalog No.S1147 Synonyms: AZD2811, INH-34

81 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 81 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 MoK1S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M1v4TlAuPTByIH7N M325ZVQ5yqCq NEnEe3JKSzVyPUK1JI5O M3zk[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mke3OlU6Lz5{NUK3O|Y2QTxxYU6=
LNCaP NWLIN4hLSXCxcITvd4l{KEG|c3H5 NXn1ZoRGOC13MECgcm0> MnPoOFjDqGh? NUTaNVR3cW6mdXPld{BieG:ydH;0bYMh[2WubDDk[YF1cCC2aILveYdpKGOjc4Dhd4UuOyC3cILl[5Vt[XSrb36= M3fXT|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ3Mke3OlU6Lz5{NUK3O|Y2QTxxYU6=
LNCaP NHrVW4pHfW6ldHnvckBCe3OjeR?= NVy0TJFuPTBibl2= Mle3OFghcA>? MnjHbY5lfWOnczDtbYNzd263Y3zlbUB4cXSqIHHu[ZVo\W6rYzDt[YNp[W6rc32= NF:3UoM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NUK3O|Y2QSd-MkWyO|c3PTl:L3G+
Ramos MonOSpVv[3Srb36gRZN{[Xl? M2fEZlUxOCCwTR?= MXWwMVczKGh? MkLsbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn NY\LZZBPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Daudi  M3TFOGZ2dmO2aX;uJGF{e2G7 M1f4RVUxOCCwTR?= Mmr5NE04OiCq MoTobY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn M4i4eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
L540 NWHSNog2TnWwY4Tpc44hSXO|YYm= M2LUSlUxOCCwTR?= NYS2SmVqOC15MjDo MnmwbY5pcWKrdIOgRZVzd3KjIFKgb4lv[XOn NXW1Onl[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
BJAJ NWnrPGpYT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXnkOZprPTByIH7N Ml;oNE04OiCq MVnpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NFzBV3U9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Ramos MX;Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NIHBOlE2ODBibl2= MWiwMVczKGh? M3vp[IlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= M1vCU|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Raji NFe5eZRIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= NXPXRndyPTByIH7N NX\sNVhKOC15MjDo MUXpcohq[mm2czDj[YxtKGe{b4f0bEB{cWewaX\pZ4FvfGy7 NX\veWJPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Daudi  Ml23S5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHPjfIQ2ODBibl2= M1nJdVAuPzJiaB?= M2X2cIlvcGmkaYTzJINmdGxiZ4Lve5RpKHOrZ37p[olk[W62bIm= NEWxWFc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
L428 M1PZUmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MVm1NFAhdk1? NYizfIluOC15MjDo MXfpcohq[mm2czDj[YxtKGe{b4f0bC=> Ml[wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
KM-H2 NGnU[FJIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3TUflUxOCCwTR?= NWKyfZhCOC15MjDo NVHnZVZjcW6qaXLpeJMh[2WubDDndo94fGh? M1zRS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
HDLM-2 NXm3d3RmT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NXT4NoJOPTByIH7N MkL4NE04OiCq MX3pcohq[mm2czDj[YxtKGe{b4f0bC=> NHjpOVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
L450 MlOyS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M321SFUxOCCwTR?= MnPDNE04OiCq NFfBS|hqdmirYnn0d{Bk\WyuIHfyc5d1cA>? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
BJAJ MUPBdI9xfG:|aYOgRZN{[Xl? MUK1NFAhdk1? MXWwMVczKGh? MoTCbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M3O1ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
Ramos MUjBdI9xfG:|aYOgRZN{[Xl? MXy1NFAhdk1? MVSwMVczKGh? MWXpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= NHTFeFM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
Raji NXPqeJRkSXCxcITvd4l{KEG|c3H5 NGHwXHE2ODBibl2= NYHvNHRPOC15MjDo NUjETYk6cW6mdXPld{BieG:ydH;zbZMhcW5iYTD0bY1mNWSncHXu[IVvfCCvYX7u[ZI> NWDCdlV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkGzO|E1PDZpPkKxN|cyPDR4PD;hQi=>
Daudi  NILsWVJCeG:ydH;zbZMhSXO|YYm= MlfaOVAxKG6P NFvNcFYxNTd{IHi= MXzpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= MmnyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF|N{G0OFYoRjJzM{exOFQ3RC:jPh?=
L428 MlS2RZBweHSxc3nzJGF{e2G7 NWXDSIlsPTByIH7N Mn;qNE04OiCq MlvibY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOTN5MUS0Okc,OjF|N{G0OFY9N2F-
KM-H2 NWXhboJ5SXCxcITvd4l{KEG|c3H5 M3fycVUxOCCwTR?= MV2wMVczKGh? MXnpcoR2[2W|IHHwc5B1d3OrczDpckBiKHSrbXWt[IVx\W6mZX70JI1idm6nch?= M3;jV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
HDLM-2 M4rYSGFxd3C2b4Ppd{BCe3OjeR?= M3;wXFUxOCCwTR?= MUewMVczKGh? MmTCbY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= NF;yRVQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MUO3NVQ1Pid-MkGzO|E1PDZ:L3G+
L450 MoHjRZBweHSxc3nzJGF{e2G7 MlPVOVAxKG6P M1fsU|AuPzJiaB?= Mni3bY5lfWOnczDhdI9xfG:|aYOgbY4h[SC2aX3lMYRmeGWwZHXueEBu[W6wZYK= M3jDRlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzM{exOFQ3Lz5{MUO3NVQ1PjxxYU6=
SW620 MUHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MVPFR|UxRTFywsGyMlEhdk1? M3y5TVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJzMkS1NFkxLz5{MUK0OVA6ODxxYU6=
HCT116 M4DjdGdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 NGDFZ2FGSzVyPUGxxtE{NjNibl2= Mn25QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjF{NEWwPVAoRjJzMkS1NFkxRC:jPh?=
MDA-MB-435 MVvHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnzvNE0yODByMDDuUS=> M{XlTVIuPSCm NX\ZcoJ1TE2VTx?= NVPtO3luUUN3ME2xNlUhdk1? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF5NUmyOkc,OjBzN{W5NlY9N2F-
MDA-MB-468 MmjuS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NFTLbJIxNTFyMECwJI5O NH;kWI4zNTViZB?= NIj3c3FFVVOR NEf5cYlKSzVyPUG0JI5O M1PETVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUe1PVI3Lz5{MEG3OVkzPjxxYU6=
MDA-MB-231 MVHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYqwMVExODByIH7N MmDENk02KGR? MkHzSG1UVw>? NGOz[ZNKSzVyPUGwOUBvVQ>? NYPQS2FzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
BT474 M{Hld2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 Mn;TNE0yODByMDDuUS=> MVGyMVUh\A>? NXTKXYtHTE2VTx?= MXLJR|UxRThibl2= NI\2Ooo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MEG3OVkzPid-MkCxO|U6OjZ:L3G+
MDA-MB-361 NHrieYlIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MWSwMVExODByIH7N MYKyMVUh\A>? MUHEUXNQ MlXDTWM2OD15MDDuUS=> MmHVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjBzN{W5NlYoRjJyMUe1PVI3RC:jPh?=
HER18 MV3Hdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NXzzU4VGOC1zMECwNEBvVQ>? NFX1N5YzNTViZB?= NXHvbFdtTE2VTx?= NF33dWZKSzVyPUKwJI5O MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zODF5NUmyOkc,OjBzN{W5NlY9N2F-
HER18 NIrDW|RCeG:ydH;zbZMhSXO|YYm= MoDmNVAxKG6P Ml7NNE8zPC92ODDo M336VWROW09? NHvTb5hqdmS3Y3XzJIFxd3C2b4Ppd{BidmRicnXkeYNmeyClbH;uc4dmdmmlIIDveIVvfGmjbB?= NWHXRWVIRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkCxO|U6OjZpPkKwNVc2QTJ4PD;hQi=>
MDA-MB-231 NX7GeGFjSXCxcITvd4l{KEG|c3H5 MYSxNFUhdk1? NGXuVJMxNzJ2L{S4JIg> M{\1NWROW09? M{TndYlv\HWlZYOgZZBweHSxc3nzJIFv\CC{ZXT1Z4V{KGOub37v[4VvcWNicH;0[Y51cWGu M3fXPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJyMUe1PVI3Lz5{MEG3OVkzPjxxYU6=
JHH-1 Mm[wS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3qxbFAvO+LCk{GwNFDDqG6P NUjL[4E4PzJiaB?= NYK2[nptTUN3ME2xO{41yrFzLkCgcm0> MWS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
JHH-2 NXfSXYx7T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEDLSFMxNjQkgKOxNFAxyqCwTR?= NEmyN4M4OiCq MYXFR|UxRTJzOD6wxtEyOC56IH7N MUW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
JHH-4 MnPjS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MmX1NE4{6oDVMUCwNOKhdk1? NIjKT484OiCq NILXTGJGSzVyPUG1OU43yrFzNj64JI5O MnO2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HuH-1 M4XXZ2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MXmwMlPjiJNzMECwxsBvVQ>? MUW3NkBp MVvFR|UxRTJ5LkRCtVUvOCCwTR?= NIX4O3A9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HuH-6 MUXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MWKwMlPjiJNzMECwxsBvVQ>? NFraR5I4OiCq MXXFR|UxRTNwN9MxNE43KG6P NHn1[ZQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
HuH-7 MVnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NX3wTGx{OC5|4pETNVAxOMLibl2= NYfPVGxPPzJiaB?= Mo\qSWM2OD14LklCtVAvOyCwTR?= Mn;NQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HLE NXvhRZd{T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml:wNE4{6oDVMUCwNOKhdk1? MX:3NkBp NV7QZ3ZwTUN3ME20OU46yrF4LkSgcm0> MoXpQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HLF MYHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MYewMlPjiJNzMECwxsBvVQ>? Ml31O|IhcA>? NHrUfplGSzVyPUGyOk4yyrFzMj6yJI5O MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTlzM{mzOUc,OTl7MUO5N|U9N2F-
PLC/PRF/5 MXHHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? Mk\0NE4{6oDVMUCwNOKhdk1? MWe3NkBp MkDwSWM2OD15Nj65xtE6Njlibl2= NF\5dJM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
SK-Hep1 NXTkUJBtT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= Ml;zNE4{6oDVMUCwNOKhdk1? NIXIUIU4OiCq MYrFR|UxRTJzLkpCtVEvOiCwTR?= MnzXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
Hep3B MVzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MV2wMlPjiJNzMECwxsBvVQ>? M2fO[|czKGh? MlPwSWM2OD15LkdCtVEvOiCwTR?= MmLvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTl7MUO5N|UoRjF7OUGzPVM2RC:jPh?=
HepG2 NHj4RoFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= Mn:3NE4{6oDVMUCwNOKhdk1? M13mNVczKGh? MV\FR|UxRTF2LkhCtVEvPyCwTR?= NHvvN5c9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUmxN|k{PSd-MUm5NVM6OzV:L3G+
Ramos NIf4fVVCeG:ydH;zbZMhSXO|YYm= M3O0TVI2NzVyL{GwNEBvVQ>? NW\DVIpiPDhiaB?= NWizU4tScW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MVO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{M{G2PEc,OTl6MkOxOlg9N2F-
Daudi  MVvBdI9xfG:|aYOgRZN{[Xl? MVuyOU82OC9zMECgcm0> MVK0PEBp MkHBbY5kemWjc3XzJJRp\SCuZY\lcJMhd2ZidHjlJINt\WG4ZXSg[o9zdXNib3[gVGFTWCCjbnSgZ4F{eGG|ZTCz M{H3N|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF7OEKzNVY5Lz5zOUiyN|E3QDxxYU6=
BALM-14 MlHBRZBweHSxc3nzJGF{e2G7 NH;VVGMyOi53L{K1M|UxKG6P NXj1XZRzPDhiaB?= M4C3Nolv[3KnYYPld{B1cGVibHX2[Yx{KG:oIITo[UBkdGWjdnXkJIZwem2|IH;mJHBCWlBiYX7kJINie3Cjc3WgNy=> NEiyfpQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUiyN|E3QCd-MUm4NlMyPjh:L3G+
BALM-27 M133R2Fxd3C2b4Ppd{BCe3OjeR?= NYryNJRwOTJwNT:yOU82OCCwTR?= MnTtOFghcA>? NWr3XoQ2cW6lcnXhd4V{KHSqZTDs[ZZmdHNib3[geIhmKGOuZXH2[YQh\m:{bYOgc4YhWEGUUDDhcoQh[2G|cHHz[UA{ MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTh{M{G2PEc,OTl6MkOxOlg9N2F-
NB4 Mk\GS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV:2[nVJOC5yMT:wMlEwOSEQvF2= NF;VWnI1QCCq MlHHbY5pcWKrdIOgZ4VtdCCpcn;3eIghe2mpbnnmbYNidnSueR?= M1HYN|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6M{[3OFg1Lz5zOEO2O|Q5PDxxYU6=
HeLa MYXGeY5kfGmxbjDBd5NigQ>? NYrPToJ{OSC3TR?= MY[yOEBpenN? MlfPTY5pcWKrdHnvckBw\iCjdYLvdoEhSiCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjlUIEh[2WubIOgZZQhOSC3TTDh[pRmeiB{NDDodpMh[nliV3XzeIVzdiCkbH;0eIlv\w>? NUXSNplYRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkC2PFQ2PDlpPkKwOlg1PTR7PD;hQi=>

... 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)
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
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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
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    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):
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    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

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