AT9283

Catalog No.S1134

For research use only.

AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.

AT9283 Chemical Structure

CAS No. 896466-04-9

Selleck's AT9283 has been cited by 24 publications

Purity & Quality Control

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Biological Activity

Description AT9283 is a potent JAK2/3 inhibitor with IC50 of 1.2 nM/1.1 nM in cell-free assays; also potent to Aurora A/B, Abl1(T315I). Phase 2.
Targets
JAK3 [1]
(Cell-free assay)
JAK2 [1]
(Cell-free assay)
Aurora A [1]
(Cell-free assay)
Aurora B [1]
(Cell-free assay)
Abl1 (T315I) [1]
(Cell-free assay)
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1.1 nM 1.2 nM ~3.0 nM ~3.0 nM 4 nM
In vitro

AT9283 leads to a clear polyploid phenotype by inhibiting the activity of Aurora B kinase in HCT116 cells with IC50 of 30 nM. Furthermore, AT9283 also produces the potent inhibition on HCT116 colony formation. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 M3Tic2N6fG:2b4jpZ4l1gSCjc4PhfS=> M{HrNFExKHSxIEG0JIRigXN? NFrzVohEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBJS1RzMU[gZ4VtdHNiYYPz[ZN{\WRiYYOgcpVu[mW{IH;mJINwdG:waXXzJIFnfGW{IEGwJJRwKDF2IHThfZMh[nliY3;sc456KG[xcn3pcoch[XO|YYmsJGlEPTB;MD6wNVLPxE1? NFjGNXU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG0N|U3Pyd-MUmxOFM2Pjd:L3G+
HCT116 M3XnS2Z2dmO2aX;uJIF{e2G7 NETFUFIyOCCvZz;r[y=> NIjnUmxEdWG6IHnuJGJCVEJxYzDtc5V{\SCkZXHybY5oKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCxNEBu\y:tZzygdI8tKEOvYYi9NE41Pc7:TR?= NHzRdWQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG0N|U3Pyd-MUmxOFM2Pjd:L3G+
HCT116 MYDGeY5kfGmxbjDhd5NigQ>? NF;VXXY2KG2pL3vn MY\DcYF5KGmwIFLBUGIw[yCvb4Xz[UBj\WG{aX7nJIh2dWGwIFjDWFEyPiClZXzsd{BifCB3IH3nM4toNCCrdjygR41igD12LkpOwG0> MlGxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzNEO1OlcoRjF7MUSzOVY4RC:jPh?=
HCT116 MYDGeY5kfGmxbjDhd5NigQ>? NGf4ToUzOCCvZz;r[y=> M1ixOmNu[XhiaX6gRmFNSi:lIH3veZNmKGKnYYLpcochcHWvYX6gTGNVOTF4IHPlcIx{KGG2IEKwJI1oN2upLDDpdEwhS22jeE24MlTPxE1? NWfuUYhpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxOFM2PjdpPkG5NVQ{PTZ5PD;hQi=>
HT-29 MYjBcpRqfHWvb4KgZZN{[Xl? MW[3NkBpenN? NFS1dI1CdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDIWE0zQSClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUCuN|g{|ryP NVXKOGFCRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OlQxQTlpPkKzOlY1ODl7PD;hQi=>
A549 NH\YfXpCdnSrdIXtc5Ih[XO|YYm= MmPNO|IhcHK| Mm\jRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwNUGy{txO NYXzdlVxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OlQxQTlpPkKzOlY1ODl7PD;hQi=>
LoVo M1rreGFvfGm2dX3vdkBie3OjeR?= MYC3NkBpenN? NEPod5hCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD61OVPPxE1? MnTOQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4NkSwPVkoRjJ|Nk[0NFk6RC:jPh?=
K562 NIfIbHlCdnSrdIXtc5Ih[XO|YYm= M4\Xb|czKGi{cx?= NH:wTGFCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDLOVYzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MT62{txO MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4NEC5PUc,OjN4NkSwPVk9N2F-
U937 MnLBRY51cXS3bX;yJIF{e2G7 NWrsSHkzPzJiaILz NGnxTGxCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDVPVM4KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;Nj63{txO NVPKV2VORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkO2OlQxQTlpPkKzOlY1ODl7PD;hQi=>
BL21 (DE3) NV3yeHJSTnWwY4Tpc44h[XO|YYm= M4TUdVMxKG2rboO= MnvUTY5pcWKrdHnvckBw\iCKaYO2MZRi\2enZDDNSWxMKGOjdHHsfZRq[yCmb33hbY4hMDFidH:gN|QxKHKnc3nkeYV{MSBqdX7rco94diCxcnnnbY4qKGW6cILld5Nm\CCrbjDFd4Np\XKrY3jpZUBkd2yrIFLMNlEhMESHMzmgZ4VtdHNidYPpcochSmOuLVfMJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkA{OCCvaX7zJIlvKHC{ZYPlcoNmKG:oIGvnZY1u[TN{UG3BWHAh[nlibHnxeYllKHOlaX70bYxt[XSrb36gZ492dnSrbnegcYV1cG:mLDDJR|UxRTBwNki1{txO NWjCfFFPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkizOVE3ODdpPkK4N|UyPjB5PD;hQi=>
Sf9 NG\We5hHfW6ldHnvckBie3OjeR?= NELDV2RDcW6maX7nJIFn\mmwaYT5JJRwKE5vdHXycYlv[WxiVFXWMYNt\WG4YXLs[UBp\XijLXjpd5Rq\GmwZTD0ZYdo\WRiaIXtZY4hUkGNMjDKTFEh\G:vYXnuJEg5PDBidH:gNVE{OiC{ZYPp[JVmeyliZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{NWmwZnXjeIVlKFOoOTDj[YxteyCkeTDJWGMh[XO|YYmsJGtlRTBwMEGx{txO MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ{NkWyNUc,Ojh4Mk[1NlE9N2F-
Sf9 MX3GeY5kfGmxbjDhd5NigQ>? M1HFfmJqdmSrbnegZYZncW6rdImgeI8hSy22ZYLtbY5idCC2aILvcYJqdi2lbHXheoFjdGViaHX4ZU1pcXO2aXTpcoUhfGGpZ3XkJIh2dWGwIFrBT|IhUkh{IIDz[ZVld2urbnHz[UBld22jaX6gLFU{PiC2bzC4NVIhemW|aXT1[ZMqKFd4NUnBM3c4PzeDL1[3PVRJKG23dHHueEBmgHC{ZYPz[YQhcW5iYnHjeYxwfmm{dYOtbY5n\WO2ZXSgV4Y6KGOnbHzzJIJ6KEmWQzDhd5NigSxiS3S9NU4{OjQQvF2= NU\LWYJoRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2NlY2OjFpPkK4OlI3PTJzPD;hQi=>
Sf9 M{DCXWZ2dmO2aX;uJIF{e2G7 NIjBWHAyOCC3TR?= NFTScFA3OCCvaX7z Moq3SIl{eGyjY3Xt[Y51KG:oIFLPSGlRYS2DVGCg[pJwdSCFLYTldo1qdmGuIITodo9u[mmwLXPs[YF3[WKuZTDo[ZhiNWirc4Tp[Ilv\SC2YXfn[YQhcHWvYX6gTmFMOiCMSEKgdJNmfWSxa3nuZZNmKGSxbXHpckApPTN4IITvJFgyOiC{ZYPp[JVmeyliV{[1PWEwXzd5N1GvSlc6PEhibYX0ZY51KGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{1qdm[nY4Tl[EBU\jliY3XscJMh[XRiMUCgeW0h[W[2ZYKgOlAhdWmwczDifUBpcWeqLYTodo92\2iydYSg[ox2 NIrIOYE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[yOlUzOSd-Mki2NlY2OjF:L3G+
HCT116 M{n4e2Z2dmO2aX;uJIF{e2G7 M133bmlvcGmkaYTpc44hd2ZiQYXyc5JiKEJia3nuZZNmKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icH;sfZBtd2mmIIDo[Y5wfHmyZTygTWM2OD1yLkCz{txO NEjGW5Y9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEmxPFA6Pid-Mki5NVgxQTZ:L3G+
DAOY M{nycZFJXFNiYYPzZZk> M2DlRpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| M{DnfVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 MmmzdWhVWyCjc4PhfS=> NEXMTmpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> M3TITlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 M3;ZV5FJXFNiYYPzZZk> MYTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSTZ5MzDj[Yxtew>? MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MX3xTHRUKGG|c3H5 M362UpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMW1EKGOnbHzz MoT6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-37 M1jJPJFJXFNiYYPzZZk> NGnDfmVyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= NHrUcYw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB-EBc1 NG\wfWhyUFSVIHHzd4F6 MYrxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS MYfxTHRUKGG|c3H5 MljydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFVvMjDPV{Bk\Wyucx?= MlvCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 MkD4dWhVWyCjc4PhfS=> NV\XeJhCeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH NEfYcnhyUFSVIHHzd4F6 Ml;YdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NULOPXRkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 MYDxTHRUKGG|c3H5 M{\Td5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= MoX4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
LAN-5 NV7SbZMxeUiWUzDhd5NigQ>? Mm\EdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| M3Ozb|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MlHFdWhVWyCjc4PhfS=> MljwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy| NHn3PVM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 MnrYdWhVWyCjc4PhfS=> Mk[2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? M3:4OVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
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RD NHzUOXByUFSVIHHzd4F6 NXPN[lBveUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| M1PpPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) Mn3ndWhVWyCjc4PhfS=> MXTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? M3zo[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
fibroblast cells NUe2NVRreUiWUzDhd5NigQ>? NID3RmRyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
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Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 21430070
In vivo In HCT116 human colon carcinoma xenograft bearing mice, AT9283 treatment (15 mg/kg and 20 mg/kg) for 16 days results in a significant tumor growth inhibition of 67% and 76%, respectively. In addition, AT9283 also exhibits a significantly longer half-life in tumors(2.5 hours) compared with plasma (0.5 hour) and modest oral bioavailability in mice (Fp.o. = 24%). [1]

Protocol (from reference)

Kinase Assay:

[1]

  • Aurora A and Aurora B Kinase Assays:

    Assays for Aurora A and B are performed in a DELFIA format. Aurora A enzyme is incubated with AT9283 and 3 μM cross-tide substrate (biotin-CGPKGPGRRGRRRTSSFAEG) in 10 mM MOPS, pH 7, 0.1 mg/mL BSA, 0.001% Brij-35, 0.5% glycerol, 0.2 mM EDTA, 10 mM MgCl2, 0.01% β-mercaptoethanol, 15 μM ATP, and 2.5% DMSO. Aurora B enzyme is incubated with AT9283, 3 μM of the above substrate in 25 mM Tris, pH 8.5, 5 mM MgCl2, 0.1 mg/mL BSA, 0.025% Tween-20, 1 mM DTT, 15 μM ATP, and 2.5% DMSO. Reactions are allowed to proceed for 60 minutes and 45-90 minutes for Aurora A and Aurora B, respectively, before quenching with EDTA. The reaction mixtures are then transferred to a neutravidin-coated plate, and phosphorylated peptide is quantified by means of a phospho-specific antibody and a europium labeled secondary antibody using time-resolved fluorescence (excitation, 337 nm; emission, 620 nm). IC50 values for the control compounds are 92 nM (Aurora A assay) and 17 nM (Aurora B).

Cell Research:

[1]

  • Cell lines: HCT 116 cells
  • Concentrations: 1 nM - 10 μM
  • Incubation Time: 72 hours
  • Method:

    HCT 116 cells are cultured in DMEM + 10% FBS + GLUTAMAX I. Black 96-well flat-bottomed (clear) tissue culture treated plates are seeded in 200 μL of medium and incubated for approximately 16 hours at 37°C in a humidified atmosphere of 5% CO2 in air. Cells are treated with test compound at nine different concentrations (spanning 1 nM to 10 μM, plus DMSO vehicle control) and then incubated for 72 hours. Polyploidy morphological observations of the cells are then noted. The concentration of AT9283 required to produce a distinct polyploid phenotype is reported. Cells are seeded at a concentration of 75−100 cells/mL relevant culture media onto 6- or 24-well tissue culture plates and allowed to recover for 16 hours. Test compound (11 concentrations spanning 0.1 nM to 10 μM) or vehicle control (DMSO) is added to duplicate wells to give a final DMSO concentration of 0.1%. Following compound addition, colonies are allowed to grow between 10 and 14 days for optimum discrete colony counting. Colonies are fixed in 2 mL of Carnoys fixative (25% acetic acid, 75% MeOH) and stained in 2 mL of 0.4% w/v crystal violet. The numbers of colonies in each well is counted. IC50 values are calculated by sigmoidal dose-response (variable slope) IC50 curves using Prism Graphpad software.

Animal Research:

[1]

  • Animal Models: HCT116 cells are injected s.c. Into the hind flank of male BALB/c mice.
  • Dosages: 15 mg/kg and 20 mg/kg
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG 300+ddH2O
For best results, use promptly after mixing.

5mg/mL

Chemical Information

Molecular Weight 381.43
Formula

C19H23N7O2

CAS No. 896466-04-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC1NC(=O)NC2=C(NN=C2)C3=NC4=C(N3)C=C(C=C4)CN5CCOCC5

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01145989 Completed Drug: AT9283 Multiple Myeloma NCIC Clinical Trials Group|Astex Pharmaceuticals Inc.|Canadian Cancer Trials Group June 15 2010 Phase 2
NCT00443976 Completed Drug: Aurora kinase inhibitor AT9283 Non-Hodgkins Lymphoma|Unspecified Adult Solid Tumor Protocol Specific NCIC Clinical Trials Group|Astex Pharmaceuticals Inc.|Canadian Cancer Trials Group January 4 2007 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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