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 23 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)
Click to View More Targets
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 MkH1R5l1d3SxeHnjbZR6KGG|c3H5 MV6xNEB1dyBzNDDkZZl{ Mm\6R5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gTGNVOTF4IHPlcIx{KGG|c3Xzd4VlKGG|IH71cYJmeiCxZjDjc4xwdmmnczDh[pRmeiBzMDD0c{AyPCCmYYnzJIJ6KGOxbH;ufUBnd3KvaX7nJIF{e2G7LDDJR|UxRTBwMEGy{txO NFTZN249[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG0N|U3Pyd-MUmxOFM2Pjd:L3G+
HCT116 M1vSXWZ2dmO2aX;uJIF{e2G7 NIS4eoIyOCCvZz;r[y=> MW\DcYF5KGmwIFLBUGIw[yCvb4Xz[UBj\WG{aX7nJIh2dWGwIFjDWFEyPiClZXzsd{BifCBzMDDt[{9s\yxicH:sJGNu[Xh;MD60Oe69VQ>? NWHnd|JjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxOFM2PjdpPkG5NVQ{PTZ5PD;hQi=>
HCT116 MnrySpVv[3Srb36gZZN{[Xl? M4DOTFUhdWdxa3e= MmX3R41igCCrbjDCRWxDN2NibX;1d4Uh[mWjcnnu[{BpfW2jbjDIR3QyOTZiY3XscJMh[XRiNTDt[{9s\yxiaY[sJGNu[Xh;ND65{txO MkHzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzNEO1OlcoRjF7MUSzOVY4RC:jPh?=
HCT116 MVTGeY5kfGmxbjDhd5NigQ>? MlvtNlAhdWdxa3e= NYX6NlQxS22jeDDpckBDSUyEL3OgcY92e2ViYnXhdolv\yCqdX3hckBJS1RzMU[gZ4VtdHNiYYSgNlAhdWdxa3esJIlxNCCFbXH4QVgvPM7:TR?= MmnQQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzNEO1OlcoRjF7MUSzOVY4RC:jPh?=
HT-29 M3qzZmFvfGm2dX3vdkBie3OjeR?= MkL1O|IhcHK| MWjBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKVD2yPUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwM{iz{txO MkPnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4NkSwPVkoRjJ|Nk[0NFk6RC:jPh?=
A549 M2nyW2FvfGm2dX3vdkBie3OjeR?= NF7Db2w4OiCqcoO= Ml\4RY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQUW0PUBk\WyuczDh[pRmeiB5MjDodpMh[nliTWTUJIF{e2G7LDDJR|UxRTBwNUGy{txO NHvRW4k9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2OFA6QSd-MkO2OlQxQTl:L3G+
LoVo NVPaVHBHSW62aYT1cY9zKGG|c3H5 M1jDUVczKGi{cx?= MYDBcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCOb2\vJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OC53NUROwG0> MlHWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN4NkSwPVkoRjJ|Nk[0NFk6RC:jPh?=
K562 M1PG[mFvfGm2dX3vdkBie3OjeR?= M4rseFczKGi{cx?= MV;BcpRqfHWvb4KgZYN1cX[rdImgZYdicW6|dDDoeY1idiCNNU[yJINmdGy|IHHmeIVzKDd{IHjyd{BjgSCPVGSgZZN{[XluIFnDOVA:OS54zszN M1\GbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[0NFk6Lz5{M{[2OFA6QTxxYU6=
U937 Ml3YRY51cXS3bX;yJIF{e2G7 MkH6O|IhcHK| NXHEPIZPSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[uO:69VQ>? MYC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzZ4NEC5PUc,OjN4NkSwPVk9N2F-
BL21 (DE3) MYfGeY5kfGmxbjDhd5NigQ>? MUSzNEBucW6| NXW3bnY{UW6qaXLpeIlwdiCxZjDIbZM3NXSjZ3fl[EBOTUyNIHPheIFtgXSrYzDkc41icW5iKEGgeI8hOzRyIILld4llfWW|KTCoeY5sdm:5bjDvdolocW5rIHX4dJJme3OnZDDpckBGe2OqZYLpZ4hq[SClb3zpJGJNOjFiKFTFN{kh[2WubIOgeZNqdmdiQnPsMWdNKGG|IIP1ZpN1emG2ZTDt[YF{fXKnZDDh[pRmeiB|MDDtbY5{KGmwIIDy[ZNmdmOnIH;mJHto[W2vYUOyVH1CXFBiYomgcIlyfWmmIIPjbY51cWyuYYTpc44h[2:3boTpcochdWW2aH;kMEBKSzVyPUCuOlg2|ryP NIPISJo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEO1NVYxPyd-MkizOVE3ODd:L3G+
Sf9 MkfUSpVv[3Srb36gZZN{[Xl? MmLtRolv\GmwZzDh[oZqdmm2eTD0c{BPNXSncn3pcoFtKFSHVj3jcIVifmGkbHWgbIV5[S2qaYP0bYRqdmVidHHn[4VlKGi3bXHuJGpCUzJiSlixJIRwdWGrbjCoPFQxKHSxIEGxN|IhemW|aXT1[ZMqKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{1qdm[nY4Tl[EBU\jliY3XscJMh[nliSWTDJIF{e2G7LDDL[F0xNjBzMd88US=> NHrIW4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[yOlUzOSd-Mki2NlY2OjF:L3G+
Sf9 NWe0PGRQTnWwY4Tpc44h[XO|YYm= NYnOXlZnSmmwZHnu[{Bi\m[rbnn0fUB1dyCFLYTldo1qdmGuIITodo9u[mmwLXPs[YF3[WKuZTDo[ZhiNWirc4Tp[Ilv\SC2YXfn[YQhcHWvYX6gTmFMOiCMSEKgdJNmfWSxa3nuZZNmKGSxbXHpckApPTN4IITvJFgyOiC{ZYPp[JVmeyliV{[1PWEwXzd5N1GvSlc6PEhibYX0ZY51KGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{1qdm[nY4Tl[EBU\jliY3XscJMh[nliSWTDJIF{e2G7LDDL[F0yNjN{M988US=> MWC8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDZ{NkWyNUc,Ojh4Mk[1NlE9N2F-
Sf9 NXfvZ4pSTnWwY4Tpc44h[XO|YYm= NYT4WnhwOTBidV2= M3PvU|YxKG2rboO= MX7EbZNxdGGlZX3lcpQhd2ZiQl;ETXB[NUGWUDDmdo9uKENvdHXycYlv[WxidHjyc41jcW5vY3zlZZZi[mynIHjlfIEucGm|dHnkbY5mKHSjZ3fl[EBpfW2jbjDKRWszKEqKMjDwd4V2\G:taX7hd4Uh\G:vYXnuJEg2OzZidH:gPFEzKHKnc3nkeYV{MSCZNkW5RU9YPzd5QT;GO|k1UCCvdYThcpQh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzMYlv\mWldHXkJHNnQSClZXzsd{BifCBzMDD1UUBi\nSncjC2NEBucW6|IHL5JIhq\2hvdHjyc5VocHC3dDDmcJU> NI\jdHY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OE[yOlUzOSd-Mki2NlY2OjF:L3G+
HCT116 M1jNcmZ2dmO2aX;uJIF{e2G7 MkPHTY5pcWKrdHnvckBw\iCDdYLvdoEhSiCtaX7hd4UhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJJJm\HWldHnvckBqdiCyb3z5dIxwcWRicHjlco91gXCnLDDJR|UxRTBwMEROwG0> Mmf6QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh7MUiwPVYoRjJ6OUG4NFk3RC:jPh?=
DAOY NIftdnVyUFSVIHHzd4F6 NFjOcnpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiRFHPXUBk\Wyucx?= MU[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SJ-GBM2 MUXxTHRUKGG|c3H5 MlzQdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= M2XNbVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
A673 NVfTfIJIeUiWUzDhd5NigQ>? MnXZdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEF4N{OgZ4VtdHN? NXvsWnUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MXjxTHRUKGG|c3H5 MoDVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NUeycVJ{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 NEH0[ldyUFSVIHHzd4F6 NGT5Z4RyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStN|ch[2WubIO= MlnJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 MlvkdWhVWyCjc4PhfS=> NFe5N4ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> M1vZPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS M1;GcJFJXFNiYYPzZZk> Mo\xdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFVvMjDPV{Bk\Wyucx?= MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 MXLxTHRUKGG|c3H5 NYDwVHNzeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPhc5MuOiClZXzsdy=> NEnpS209[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MXfxTHRUKGG|c3H5 NHHn[W9yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1UUCClZXzsdy=> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB1643 Mnm2dWhVWyCjc4PhfS=> M4HzN5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQkG2OFMh[2WubIO= NVS0c41pRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NVzZNnp1eUiWUzDhd5NigQ>? MljwdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NWS2T5J[RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 Mkn4dWhVWyCjc4PhfS=> NH3VWWhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= M37Ec|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 MVrxTHRUKGG|c3H5 MnzCdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? NXLwNXg4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M2TlOZFJXFNiYYPzZZk> MX3xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhV0iVLUWwJINmdGy| MnL1QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD M33YZpFJXFNiYYPzZZk> MlnjdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ M3rVbFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M4fkdJFJXFNiYYPzZZk> NUDzZWpJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz M3fnV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
fibroblast cells MXrxTHRUKGG|c3H5 MUnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5Ih[2:wdILvcEBJcCC5aXzkJJR6eGViZnnido9jdGG|dDDj[Yxtew>? MWO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh41 NF:0W3ByUFSVIHHzd4F6 NX\z[oVJeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= M4jsVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC MoHCdWhVWyCjc4PhfS=> MlTSdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2PQzDj[Yxtew>? NEH3TVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
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

DMSO 76 mg/mL
(199.25 mM)
Ethanol 38 mg/mL
(99.62 mM)
Water Insoluble

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 2022-01-17)

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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