AT9283

For research use only.

Catalog No.S1134

22 publications

AT9283 Chemical Structure

CAS No. 896466-04-9

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.

Selleck's AT9283 has been cited by 22 publications

Purity & Quality Control

Choose Selective JAK Inhibitors

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)
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 NX;seZp5S3m2b4TvfIlkcXS7IHHzd4F6 NGrXcY0yOCC2bzCxOEBl[Xm| MVHDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDIR3QyOTZiY3XscJMh[XO|ZYPz[YQh[XNiboXtZoVzKG:oIHPvcI9vcWW|IHHmeIVzKDFyIITvJFE1KGSjeYOgZpkh[2:ub375JIZwem2rbnegZZN{[XluIFnDOVA:OC5yMUNOwG0> NUjK[|dERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUmxOFM2PjdpPkG5NVQ{PTZ5PD;hQi=>
HCT116 MVjGeY5kfGmxbjDhd5NigQ>? NXTQdIpMOTBibXevb4c> MnXPR41igCCrbjDCRWxDN2NibX;1d4Uh[mWjcnnu[{BpfW2jbjDIR3QyOTZiY3XscJMh[XRiMUCgcYcwc2duIIDvMEBEdWG6PUCuOFXPxE1? MXu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8yQTF2M{W2O{c,OTlzNEO1Olc9N2F-
HCT116 NYi1OJQ6TnWwY4Tpc44h[XO|YYm= NVfJfJZYPSCvZz;r[y=> MkHWR41igCCrbjDCRWxDN2NibX;1d4Uh[mWjcnnu[{BpfW2jbjDIR3QyOTZiY3XscJMh[XRiNTDt[{9s\yxiaY[sJGNu[Xh;ND65{txO NILBXpA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOUG0N|U3Pyd-MUmxOFM2Pjd:L3G+
HCT116 NXzaTZhOTnWwY4Tpc44h[XO|YYm= Ml3LNlAhdWdxa3e= NIHaNVhEdWG6IHnuJGJCVEJxYzDtc5V{\SCkZXHybY5oKGi3bXHuJGhEXDFzNjDj[YxteyCjdDCyNEBu\y:tZzygbZAtKEOvYYi9PE41|ryP Ml7PQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTlzNEO1OlcoRjF7MUSzOVY4RC:jPh?=
HT-29 NWXpUVVxSW62aYT1cY9zKGG|c3H5 MUi3NkBpenN? MlnCRY51cXS3bX;yJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iSGStNlkh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IF3UWEBie3OjeTygTWM2OD1yLkO4N:69VQ>? NHXlR4I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2OFA6QSd-MkO2OlQxQTl:L3G+
A549 MkDQRY51cXS3bX;yJIF{e2G7 NXnEXWxrPzJiaILz NF;obHhCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBOVQ6KGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD61NVLPxE1? M1jkZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[0NFk6Lz5{M{[2OFA6QTxxYU6=
LoVo M2L3U2FvfGm2dX3vdkBie3OjeR?= NYS1[Wx[PzJiaILz NHzwOHZCdnSrdIXtc5Ih[WO2aY\peJkh[WejaX7zeEBpfW2jbjDMc3ZwKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDNWHQh[XO|YYmsJGlEPTB;MD61OVPPxE1? M{S1bFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Nk[0NFk6Lz5{M{[2OFA6QTxxYU6=
K562 NGnNPZZCdnSrdIXtc5Ih[XO|YYm= NV7mcY5bPzJiaILz NYnwd3BoSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gT|U3OiClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPUGuOu69VQ>? NETxRVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2OFA6QSd-MkO2OlQxQTl:L3G+
U937 MVnBcpRqfHWvb4KgZZN{[Xl? M4i2UVczKGi{cx?= NU[4R3dHSW62aYT1cY9zKGGldHn2bZR6KGGpYXnud5QhcHWvYX6gWVk{PyClZXzsd{Bi\nSncjC3NkBpenNiYomgUXRVKGG|c3H5MEBKSzVyPU[uO:69VQ>? NIHkcZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{[2OFA6QSd-MkO2OlQxQTl:L3G+
BL21 (DE3) M4P0O2Z2dmO2aX;uJIF{e2G7 NYLKNlB3OzBibXnudy=> NEPPR|JKdmirYnn0bY9vKG:oIFjpd|YufGGpZ3XkJG1GVEtiY3H0ZYx6fGmlIHTvcYFqdiBqMTD0c{A{PDBicnXzbYR2\XNrIDj1cotvd3ewIH;ybYdqdiliZYjwdoV{e2WmIHnuJGV{[2incnnjbIliKGOxbHmgRmwzOSBqRFWzLUBk\WyuczD1d4lv\yCEY3ytS2wh[XNic4Xid5Rz[XSnIH3lZZN2emWmIHHmeIVzKDNyIH3pcpMhcW5icILld4Vv[2Vib3[gX4didW2jM{LQYWFVWCCkeTDsbZF2cWRic3PpcpRqdGyjdHnvckBkd3WwdHnu[{Bu\XSqb3SsJGlEPTB;MD62PFXPxE1? MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDN3MU[wO{c,Ojh|NUG2NFc9N2F-
Sf9 NYfPOnpnTnWwY4Tpc44h[XO|YYm= NH7RZnZDcW6maX7nJIFn\mmwaYT5JJRwKE5vdHXycYlv[WxiVFXWMYNt\WG4YXLs[UBp\XijLXjpd5Rq\GmwZTD0ZYdo\WRiaIXtZY4hUkGNMjDKTFEh\G:vYXnuJEg5PDBidH:gNVE{OiC{ZYPp[JVmeyliZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{NWmwZnXjeIVlKFOoOTDj[YxteyCkeTDJWGMh[XO|YYmsJGtlRTBwMEGx{txO NWC3U49{RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki2NlY2OjFpPkK4OlI3PTJzPD;hQi=>
Sf9 MV7GeY5kfGmxbjDhd5NigQ>? NFW1bJFDcW6maX7nJIFn\mmwaYT5JJRwKENvdHXycYlv[WxidHjyc41jcW5vY3zlZZZi[mynIHjlfIEucGm|dHnkbY5mKHSjZ3fl[EBpfW2jbjDKRWszKEqKMjDwd4V2\G:taX7hd4Uh\G:vYXnuJEg2OzZidH:gPFEzKHKnc3nkeYV{MSCZNkW5RU9YPzd5QT;GO|k1UCCvdYThcpQh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzMYlv\mWldHXkJHNnQSClZXzsd{BjgSCLVFOgZZN{[XluIFvkQVEvOzJ|zszN M13jZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkK2OVIyLz5{OE[yOlUzOTxxYU6=
Sf9 NWPZ[Hl[TnWwY4Tpc44h[XO|YYm= M4CwV|ExKHWP NELCc5M3OCCvaX7z NYqyXHRmTGm|cHzhZ4Vu\W62IH;mJGJQTEmSWT3BWHAh\nKxbTDDMZRmem2rbnHsJJRpem:vYnnuMYNt\WG4YXLs[UBp\XijLXjpd5Rq\GmwZTD0ZYdo\WRiaIXtZY4hUkGNMjDKTFIheHOndXTvb4lv[XOnIHTvcYFqdiBqNUO2JJRwKDhzMjDy[ZNq\HWnczmgW|Y2QUFxV{e3O2EwTjd7NFigcZV1[W62IHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2ey2rbn\lZ5Rm\CCVZkmgZ4VtdHNiYYSgNVAhfU1iYX\0[ZIhPjBibXnud{BjgSCqaXfoMZRpem:3Z3jweZQh\my3 M4DOOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6NkK2OVIyLz5{OE[yOlUzOTxxYU6=
HCT116 NHnLR45HfW6ldHnvckBie3OjeR?= M3PyN2lvcGmkaYTpc44hd2ZiQYXyc5JiKEJia3nuZZNmKGmwIHj1cYFvKEiFVEGxOkBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5icH;sfZBtd2mmIIDo[Y5wfHmyZTygTWM2OD1yLkCz{txO NYfoc2hHRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki5NVgxQTZpPkK4PVE5ODl4PD;hQi=>
DAOY NYXZU4RZeUiWUzDhd5NigQ>? NWLqS5ZKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO= M1TQUlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 NFjWV4hyUFSVIHHzd4F6 M3L3fJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSj3HRm0zKGOnbHzz NX6wT4JyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
A673 NV7nOGV6eUiWUzDhd5NigQ>? M33jbJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NYH0OXE1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC M17PUZFJXFNiYYPzZZk> MojldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NWDjSGQ1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-37 MlG2dWhVWyCjc4PhfS=> NVvBfmp6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz M4W3V|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NXLPOHF4eUiWUzDhd5NigQ>? NX;4eXRIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
U-2 OS M{TwdZFJXFNiYYPzZZk> M1\OeZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCXLUKgU3Mh[2WubIO= M1PVV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Saos-2 NGjYe5VyUFSVIHHzd4F6 NGrwXIhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU3Hvd{0zKGOnbHzz MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH MnnKdWhVWyCjc4PhfS=> NUO2WnE4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPLMW4uW0hiY3XscJM> NF;qc|I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 M33XeJFJXFNiYYPzZZk> MoqydWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NWfxWXZyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NWGyeGNueUiWUzDhd5NigQ>? MkHqdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEyDTj21JINmdGy| NEPXNlM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 NFT5UnFyUFSVIHHzd4F6 M4XONpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= MX[8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh18 MnnJdWhVWyCjc4PhfS=> NIXqbJlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUnixPEBk\Wyucx?= MmrCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NXL0b4NOeUiWUzDhd5NigQ>? MkHVdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= MoTnQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD NFjVUGdyUFSVIHHzd4F6 NH7wbHlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUlSgZ4VtdHN? MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M3rMOJFJXFNiYYPzZZk> NHzSdXNyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= MnH4QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
fibroblast cells MYTxTHRUKGG|c3H5 NH;2O2VyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiY3;ueJJwdCCKaDD3bYxlKHS7cHWg[oljem:kbHHzeEBk\Wyucx?= NHXBNnE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M4L6cJFJXFNiYYPzZZk> NIXuRYZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiUni0NUBk\Wyucx?= NVKxU5ZQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NXH5SJBoeUiWUzDhd5NigQ>? M2fjNJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? MmnwQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 21430070     


AT9283 reduces MM cells viability in a dose dependent manner. Cells were treated with increasing doses of AT9283 for 72 hours and cell viability was measured by MTT assay

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

Kinase Assay:

[1]

- Collapse

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]

- Collapse
  • 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.


    (Only for Reference)
Animal Research:

[1]

- Collapse
  • 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.
    (Only for Reference)

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

* 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 381.43
Formula

C19H23N7O2

CAS No. 896466-04-9
Storage powder
in solvent
Synonyms N/A
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)
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
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

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

JAK Signaling Pathway Map

JAK Inhibitors with Unique Features

Related JAK Products

Tags: buy AT9283 | AT9283 supplier | purchase AT9283 | AT9283 cost | AT9283 manufacturer | order AT9283 | AT9283 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID