AT7519

For research use only.

Catalog No.S1524

39 publications

AT7519 Chemical Structure

CAS No. 844442-38-2

AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.

Selleck's AT7519 has been cited by 39 publications

Purity & Quality Control

Choose Selective CDK Inhibitors

Biological Activity

Description AT7519 is a multi-CDK inhibitor for CDK1, 2, 4, 6 and 9 with IC50 of 10-210 nM. It is less potent to CDK3 and little active to CDK7. AT7519 also inhibits GSK3β with IC50 of 89 nM. AT7519 induces apoptosis. Phase 2.
Targets
CDK9/CyclinT [1]
(Cell-free assay)
CDK5/p35 [1]
(Cell-free assay)
CDK2/CyclinA [1]
(Cell-free assay)
GSK-3β [1]
(Cell-free assay)
CDK4/CyclinD1 [1]
(Cell-free assay)
<10 nM 13 nM 47 nM 89 nM 100 nM
In vitro

AT7519 is an ATP competitive CDK inhibitor with a Ki value of 38 nM for CDK1. AT7519 is inactive against all non-CDK kinases with the exception of GSK3β (IC50 = 89 nM). AT7519 shows potent antiproliferative activity in a variety of human tumor cell lines with IC50 values ranging from 40 nM for MCF-7 to 940 nM for SW620 consistent with the inhibition of CDK1 and CDK2. [1] AT7519 induces dose-dependent cytotoxicity in multiple myeloma (MM) cell lines with IC50 values ranging from 0.5 to 2 μM at 48 hours, with the most sensitive cell lines being MM.1S (0.5 μM) and U266 (0.5 μM) and the most resistant MM.1R (>2 μM). It does not induce cytotoxicity in peripheral blood mononuclear cells (PBMNC). AT7519 partially overcomes the proliferative advantage conferred by IL6 and IGF-1 as well as the protective effect of bone marrow stromal cells (BMSCs). AT7519 induces rapid dephosphorylation of RNA pol II CTD at serine 2 and serine 5 sites, and leads to the inhibition of transcription, partially contributing to AT7519 induced cytotoxicity of MM cells. AT7519 induces activation of GSK-3β by down-regulating GSK-3β phosphorylation, which also contributes to AT7519 induced apoptosis independent of the inhibition of transcription. [2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 MV7BcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NYT6TIduPzJiaILz MlfORY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCKQ2SxNVYh[2WubIOgZZN{\XO|ZXSgZZMh[2WubDD2bYFjcWyrdImgZYZ1\XJiN{KgbJJ{KGK7IHHsZY1ieiCkbIXlJIF{e2G7LDDJR|UxRTBwMEiy{txO M13TXVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzF6NkW2PVEyLz5zOE[1OlkyOTxxYU6=
A2780 NVXQ[INSSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= NVzHdIQxPzJiaILz NYDHSldESW62aYDyc4xq\mW{YYTpeoUh[WO2aY\peJkh[WejaX7zeEBpfW2jbjDBNlc5OCClZXzsd{Bie3Onc4Pl[EBieyClZXzsJJZq[WKrbHn0fUBi\nSncjC3NkBpenNiYomgZYxidWG{IHLseYUh[XO|YYmsJGlEPTB;MD6zOe69VQ>? NV3UTJJxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2OVY6OTFpPkG4OlU3QTFzPD;hQi=>
MRC5 MVvBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? MXS3NkBpenN? M4jHUWFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iTWLDOUBk\WyuczDhd5Nme3OnZDDhd{Bk\WyuII\pZYJqdGm2eTDh[pRmeiB5MjDodpMh[nliYXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC57ON88US=> NFSwVIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9zOE[1OlkyOSd-MUi2OVY6OTF:L3G+
HCT116 Mm\mSpVv[3Srb36gZZN{[Xl? NH\BbHFKdmirYnn0bY9vKG:oIFPET|EhcW5iaIXtZY4hUEOWMUG2JINmdGy|IHHzd4V{e2WmIHHzJHBROS2jbIDoZUhVcHJ|MkCpJJBpd3OyaH;yfYxifGmxbh?= Mo\uQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh4NU[5NVEoRjF6NkW2PVEyRC:jPh?=
HCT116 MlvjSpVv[3Srb36gZZN{[Xl? Ml\QTY5pcWKrdHnvckBw\iCFRFuyJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDSZkhVcHJ|MkGpJJBpd3OyaH;yfYxifGmxbh?= MmrzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOTh4NU[5NVEoRjF6NkW2PVEyRC:jPh?=
HCT116 MX7GeY5kfGmxbjDhd5NigQ>? MlL2TY5pcWKrdHnvckBw\iCFRFuyJIlvKGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDOVG0pXGi{MUm5LUBxcG:|cHjvdplt[XSrb36= NUm5Zm1bRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMUi2OVY6OTFpPkG4OlU3QTFzPD;hQi=>
HCT116 NWjM[pNDS3m2b4TvfIlkcXS7IHHzd4F6 MmS4O|IhcHK| M17tbmN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJGhEXDFzNjDj[YxteyCjc4Pld5Nm\CCjczDndo94fGhiaX7obYJqfGmxbjDh[pRmeiB5MjDodpMh[nliQXzhcYFzKGKudXWgZZN{[XluIFnDOVA:OC5yON88US=> NWPDVVBkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMk[xNVU2PzFpPkK2NVE2PTdzPD;hQi=>
Sf21 M3rRcGZ2dmO2aX;uJIF{e2G7 M1vzbmlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscEBt\W6pdHigUk11\XKvaX7hcEBJcXN4LYTh[4dm\CCFRFu1M24ufGW{bXnuZYwhT1OWLYTh[4dm\CCyMkWg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPmNlEhcW6|ZXP0JINmdGy|IIXzbY5oKGirc4TvcoUhUDFiYYOgd5Vje3S{YYTlMEBMcT1yLkCxPO69VQ>? MnuxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjdzN{GwN|YoRjJ5MUexNFM3RC:jPh?=
Sf21 NH\ydpJHfW6ldHnvckBie3OjeR?= NFe1fGlKdmirYnn0bY9vKG:oIHj1cYFvKG[3bHygcIVv\3SqIFOteIVzdWmwYXygTIl{Pi22YXfn[YQhS0SNMj;OMZRmem2rbnHsJGdUXC22YXfn[YQh[3mlbHnuJGEh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnOjFiaX7z[YN1KGOnbHzzJJV{cW6pIHjpd5RwdmViSEGgZZMhe3Wkc4TyZZRmNCCNaU2wMlA1PM7:TR?= MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
sf cells M2fhSmZ2dmO2aX;uJIF{e2G7 M3HZS2lvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iTj30[ZJucW6jbDDHV3QufGGpZ3XkJGNFUzRxY4njcIlvKERzIHX4dJJme3OnZDDpckBj[WO3bH;2bZJ2eyCrbn\lZ5Rm\CC|ZjDj[YxteyxiS3m9NE4xPjgQvF2= NHToXHI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{N{G3NVA{Pid-MkexO|ExOzZ:L3G+
Sf21 NF:5[5NHfW6ldHnvckBie3OjeR?= NVTmZW5EUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBENXSncn3pcoFtKEirc{[teIFo\2WmIFPET|kw[3mlbHnuJHQyKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jJzIHnud4VkfCClZXzsd{B2e2mwZzDQSGt1cWSnIHHzJJN2[nO2cnH0[UwhU2l:MD6x{txO NYnyOnEzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Sf21 MofOSpVv[3Srb36gZZN{[Xl? NUXUTWw6UW6qaXLpeIlwdiCxZjDoeY1idiCodXzsJIxmdme2aDDDMZRmem2rbnHsJGhqezZvdHHn[4VlKEOGS{GvUk11\XKvaX7hcEBIW1RvdHHn[4VlKGO7Y3zpckBDKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jJzIHnud4VkfCClZXzsd{B2e2mwZzDobZN1d26nIFixJIF{KHO3YoP0doF1\SxiS3m9NE4yQc7:TR?= NULvUm1nRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkexO|ExOzZpPkK3NVcyODN4PD;hQi=>
Sf21 MmrtSpVv[3Srb36gZZN{[Xl? M13PZWlvcGmkaYTpc44hd2ZicnXjc41jcW6jboSgbJVu[W5iZoXscEBt\W6pdHigR{11\XKvaX7hcEBJcXN4LYTh[4dm\CCFRFuyM24ufGW{bXnuZYwhT1OWLYTh[4dm\CCleXPsbY4hTSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z{MTDpcpNm[3RiY3XscJMhfXOrbnegbIl{fG:wZTDINUBieyC|dXLzeJJifGVuIFvpQVAvPTIQvF2= MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
Sf21 MUPGeY5kfGmxbjDhd5NigQ>? NWrKc29CUW6qaXLpeIlwdiCxZjDy[YNwdWKrbnHueEBpfW2jbjDmeYxtKGynbnf0bEBENXSncn3pcoFtKEirc{[teIFo\2WmIFPET|cw[3mlbHnuJGgwVi22ZYLtbY5idCCJU2SteIFo\2WmIF3BWFEh\XiycnXzd4VlKGmwIHLhZ5Vtd3[rcoXzJIlv\mWldHXkJHNnOjFiaX7z[YN1KGOnbHzzJJV{cW6pIHPkb|che3Wkc4TyZZRmKHCncITp[IUtKEurPUKuPO69VQ>? MXy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPzF5MUCzOkc,OjdzN{GwN|Y9N2F-
TC32 M1HWWZFJXFNiYYPzZZk> MlnNdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFSFM{KgZ4VtdHN? M4PIV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY NFu5T2JyUFSVIHHzd4F6 M1KySZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| NYHkNHlXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 M{DRS5FJXFNiYYPzZZk> NFu2U4ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1qtS2JOOiClZXzsdy=> MVS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
A673 NFLMR4lyUFSVIHHzd4F6 M17DdZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| NHfRS2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC NFHGcIZyUFSVIHHzd4F6 MlLodWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= NESwU449[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 MX3xTHRUKGG|c3H5 NX3hR|JieUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVM4KGOnbHzz MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 M3TlXpFJXFNiYYPzZZk> MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJvRVLjNUBk\Wyucx?= NX;vXmFGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 MX3xTHRUKGG|c3H5 MlrhdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= M1PIS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-SH NUfWZY9reUiWUzDhd5NigQ>? M4S1b5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz M{DjSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-12 MkfodWhVWyCjc4PhfS=> NHjBdVdyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQmStNVIh[2WubIO= NWfG[otiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 M1PDV5FJXFNiYYPzZZk> NWPNToVpeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NEfqXW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
RD NVrYUW5ReUiWUzDhd5NigQ>? MlHzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ MnyxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) M{LuTpFJXFNiYYPzZZk> MWLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVUdiNkOgLFYuXEdiUjmgZ4VtdHN? NEHlTnM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 M17JbpFJXFNiYYPzZZk> NWjG[IxNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= NEnMTG49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
A673 NVLybG5weUiWUzDhd5NigQ>? NFXDWXlyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBCPjd|IHPlcIx{MQ>? MWG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC MWHxTHRUKGG|c3H5 M3PiVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NFX6TFY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 NV36[IIyeUiWUzDhd5NigQ>? M4HMXpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTF{IHPlcIx{ Ml[yQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
DAOY MmPYdWhVWyCjc4PhfS=> NFe5OmpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBFSU:\IHPlcIx{ MlfaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SJ-GBM2 MojYdWhVWyCjc4PhfS=> NX\XboFPeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= M1XJVFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
BT-37 NXrzTmZOeUiWUzDhd5NigQ>? M{f1cJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJGJVNTN5IHPlcIx{ MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
TC32 NFXrWYdyUFSVIHHzd4F6 NUfxVlhueUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhXEN|MjDj[Yxtew>? M2C2S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
U-2 OS M3fj[JFJXFNiYYPzZZk> M{m4V5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHUuOiCRUzDj[Yxtew>? NInZXHA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 NGHLXYxyUFSVIHHzd4F6 NY[4ZYJkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? Ml7OQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD MnLudWhVWyCjc4PhfS=> M1TiZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJFKGOnbHzz MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MlLTdWhVWyCjc4PhfS=> NFzpRY5yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDNyIHPlcIx{ MlLWQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Saos-2 NGrY[YdyUFSVIHHzd4F6 MWHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> MnHyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
OHS-50 NYLTUVVSeUiWUzDhd5NigQ>? NHrwUFhyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBQUFNvNUCgZ4VtdHN? NFjkSms9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MnrQdWhVWyCjc4PhfS=> NXPzSplkeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3TTEBk\Wyucx?= M2fQUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
HEI-OC1 M1jQOWZ2dmO2aX;uJIF{e2G7 MneyVJJwfGWldHnvckBi\2GrboP0JINqe3CuYYTpck1qdmS3Y3XkJINmdGxiZHXheIghcW5ibnXvcoF1[WxibX;1d4UhUEWLLV;DNUBk\WyuczDhd5Nme3OnZDDhd{Bz\WS3Y4Tpc44hcW5iY3HzdIF{\S1|L{egZYN1cX[rdImsJGVEPTB;MD6zPO69VQ>? NHzPfVI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEC5NVkyPSd-M{CwPVE6OTV:L3G+
MIAPaCa2 NHPD[G9CdnSrcILvcIln\XKjdHn2[UBie3OjeR?= Mk\VO|IhcHK| MX\BcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKE2LQWDhR4EzKGOnbHzzJIFnfGW{IEeyJIhzeyCkeTDwdoV{fG:kbIXlJIF{e2G7LDDJR|UxRTBwNEGx{txO M3rTNVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{SzPVU1Lz5|MEO0N|k2PDxxYU6=
AsPC1 MVnBcpRqeHKxbHnm[ZJifGm4ZTDhd5NigQ>? NIH0WnU4OiCqcoO= M4\ZXmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iQYPQR|Eh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIDy[ZN1d2KudXWgZZN{[XluIFnDOVA:OC53M{ROwG0> NVLhOFV3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFM6PTRpPkOwN|Q{QTV2PD;hQi=>
SUIT2 NYW0VpJZSW62aYDyc4xq\mW{YYTpeoUh[XO|YYm= MXK3NkBpenN? M1jvcmFvfGmycn;sbYZmemG2aY\lJIFkfGm4aYT5JIFo[Wmwc4SgbJVu[W5iU2XJWFIh[2WubIOgZYZ1\XJiN{KgbJJ{KGK7IIDy[ZN1d2KudXWgZZN{[XluIFnDOVA:OC53NUhOwG0> M1LXVVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{SzPVU1Lz5|MEO0N|k2PDxxYU6=
BxPC3 Mm\oRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? M3zEcVczKGi{cx?= MkLFRY51cXC{b3zp[oVz[XSrdnWgZYN1cX[rdImgZYdicW6|dDDoeY1idiCEeGDDN{Bk\WyuczDh[pRmeiB5MjDodpMh[nlicILld5Rw[my3ZTDhd5NigSxiSVO1NF0xNjZ2zszN NY\BbGJQRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{CzOFM6PTRpPkOwN|Q{QTV2PD;hQi=>
S2-013 Mm\hRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NELhOVk4OiCqcoO= MYPBcpRqeHKxbHnm[ZJifGm4ZTDhZ5Rqfmm2eTDh[4FqdnO2IHj1cYFvKFN{LUCxN{Bk\WyuczDh[pRmeiB5MjDodpMh[nlicILld5Rw[my3ZTDhd5NigSxiSVO1NF0zNjd5zszN MnvVQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NEO5OVQoRjNyM{SzPVU1RC:jPh?=
Sf21 MoTFSpVv[3Srb36gZZN{[Xl? MYLJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKG[3bHytcIVv\3SqIFOteIVzdWmwYXygTIl{Pi22YXfn[YQhS0SNOT;oeY1idiCodXzsMYxmdme2aDD1cpRi\2enZDDjfYNtcW5iVEGg[ZhxemW|c3XkJIlvKGKjY4Xsc5ZqenW|IHnu[oVkfGWmIGPmNlEhcW6|ZXP0JINmdGy|IIXzbY5oKFCGS4Tp[IUh[XNic4Xid5Rz[XSnLDDJR|UxRDBwMEJOwG0> NGPBSnY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW0N|Q1OCd-M{C1OFM1PDB:L3G+
Sf21 NH7IeFhHfW6ldHnvckBie3OjeR?= NYrQVYZFOiCqcoO= MmjUTY5pcWKrdHnvckBw\iC{ZXPvcYJqdmGwdDDmeYxtNWynbnf0bEBpfW2jbjDDMZRmem2rbnHsJGhqezZvdHHn[4VlKEOGS{GvbJVu[W5iZoXscE1t\W6pdHigUk11\XKvaX7hcEBIW1RvdHHn[4VlKEO7Y3zpckBDKGW6cILld5Nm\CCrbjDiZYN2dG:4aYL1d{Bqdm[nY4Tl[EBU\jJzIHnud4VkfCClZXzsd{B2e2mwZzDobZN1d26nIFixJIF{KHO3YoP0doF1\SCvZXHzeZJm\CCjZoTldkAzKGi{czDpckBxemW|ZX7j[UBw\iCpYX3tZXs{OlCfIFHUVEBjNCCLQ{WwQVAvOjIQvF2= M13KOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUSzOFQxLz5|MEW0N|Q1ODxxYU6=
Sf21 NWLhVmNKTnWwY4Tpc44h[XO|YYm= NGLsUZZKdmirYnn0bY9vKG:oIILlZ49u[mmwYX70JIh2dWGwIH\1cIwudGWwZ4ToJGMufGW{bXnuZYwhUGm|Nj30ZYdo\WRiQ1TLN{9nfWyuLXzlcod1cCCqdX3hckBPNXSncn3pcoFtKEeVVD30ZYdo\WRiQ4njcIlvKEViZYjwdoV{e2WmIHnuJIJi[3Wub4\pdpV{KGmwZnXjeIVlKFOoMkGgbY5{\WO2IHPlcIx{KHW|aX7nJIhqe3SxbnWgTFEh[XNic4Xid5Rz[XSnLDDJR|UxRTBwM{dOwG0> NHrLR2g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEW0N|Q1OCd-M{C1OFM1PDB:L3G+
Sf21 NInLb5lHfW6ldHnvckBie3OjeR?= MYXJcohq[mm2aX;uJI9nKHKnY3;tZolv[W62IHj1cYFvKENvdHXycYlv[WxiSHnzOk11[WepZXSg[pVtdCCuZX7neIghS0SNNz;1cpRi\2enZDDy[YNwdWKrbnHueEBnfWyuIHzlcod1cCCqdX3hckBEgWOuaX6gTE9PNXSncn3pcoFtKEeVVD30ZYdo\WRicnXjc41jcW6jboSg[pVtdCCuZX7neIghcHWvYX6gUWFVOSCneIDy[ZN{\WRiaX6gZoFkfWyxdnnyeZMhcW6oZXP0[YQhW2Z{MTDpcpNm[3RiY3XscJMhfXOrbnegZ4RsPyCyZYD0bYRmKGG|IIP1ZpMtKEmFNUC9Nk41|ryP MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODV2M{S0NEc,OzB3NEO0OFA9N2F-
HCT116 Mn6zRY51cXC{b3zp[oVz[XSrdnWgZZN{[Xl? NVi5PJplPzJiaILz NGrYO4NCdnSrcILvcIln\XKjdHn2[UBi[3Srdnn0fUBi\2GrboP0JIh2dWGwIFjDWFEyPiClZXzsd{Bie3Onc4Pl[EBieyC{ZXT1Z5Rqd25iaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhPzJiaILzJIJ6KGOnbHygeIl1\XJiZ3zvMYJie2WmIHz1cYlv\XOlZX7j[UBie3OjeTygTWM2OD1yLkGzNu69VQ>? MXW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{OTF5NUCxNEc,OzFzN{WwNVA9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell viability; 

PubMed: 20101221     


MM cell lines (MM.1S, U266, OPM1, RPMI, LR5, DOX 40, MM.1R) and primary CD138+ MM cells from five different patients were cultured in the presence of increasing doses of AT7519 for 48 hours. The effect of AT7519 was determined by MTT assay. IC50 ranged from 0.5 to 2 μM.

20101221
Western blot
CDK1 / CDK2 / CDK4 / Cyclin B1 / Cyclin E / CDK9 / CDK5 / CDK6 / Cyclin D1 / Cyclin A ; 

PubMed: 20101221     


MM.1S cells were incubated with AT7519 0.5 μM. At indicated time points, cells were harvested and whole lysates were subjected to Western blotting using the antibodies indicated.

20101221
In vivo A twice daily dosing of AT7519 (9.1 mg/kg) causes tumor regression of both early-stage and advanced-stage s.c. tumors in the HCT116 and HT29 colon cancer xenograft models. [1] AT7519 treatment (15 mg/kg) inhibits tumor growth and prolongs the median overall survival of mice in the human MM xenograft mouse model in association with increased caspase 3 activation. [2]

Protocol

Kinase Assay:[1]
- Collapse

In vitro Kinase Assays:

Kinase assays for CDK1, CDK2 and GSK3-β are all carried out in a radiometric filter binding format. Assays for CDK5 are in DELFIA format and for CDKs 4 and 6 in ELISA format. For CDKs 1 and 2, the relevant CDK and 0.12 μg/mL Histone H1 are incubated in 20 mM MOPS, pH 7.2, 25 mM β-glycerophosphate, 5 mM EDTA, 15 mM MgCl2, 1 mM sodium orthovanadate, 1 mM DTT, 0.1 mg/mL BSA, 45 μM ATP (0.78 Ci/mmol) and different concentrations of AT7519 for 2 or 4 hours respectively. For GSK3-β, the relevant enzyme and 5 μM glycogen synthase peptide 2 along with 10 mM MOPS pH 7.0, 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 (2.31 Ci/mmol) and different concentrations of AT7519 are incubated for 3 hours. Assay reactions are stopped by adding an excess of orthophosphoric acid and filtered using Millipore MAPH filter plates. The plates are then washed, scintillant added and radioactivity measured by scintillation counting on a Packard TopCount. For CDK5, CDK5/p35 and 1μM of a biotinylated Histone H1 peptide (Biotin-PKTPKKAKKL) are incubated in 25 mM Tris-HCl, pH 7.5, 2.5 mM MgCl2, 0.025% Brij-35, 0.1 mg/mL BSA, 1 mM DTT, 15 μM ATP and different concentrations of AT7519 for 30 minutes. Assay reactions are stopped using EDTA, transferred to Neutravidin-coated plates and phosphorylated peptide quantified by means of a rabbit phospho-cdk1 substrate polyclonal antibody and DELFIA europium-labelled anti-rabbit IgG secondary antibody using time-resolved fluorescence at λex=335nm, λem=620nm. For CDK 4 and 6 assays, plates are coated with GST- pRb769-921 and blocked with Superblock. CDK4 or 6 is incubated with 15 mM MgCl2, 50 mM HEPES, pH 7.4, 1 mM DTT, 1 mM EGTA, pH 8.0, 0.02% Triton X-100, 2.5% DMSO and different concentrations of AT7519; the reaction is initiated by addition of ATP. After 30 minutes, reactions are stopped by the addition of 0.5 M EDTA pH 8.0. Plates are then washed and incubated for one hour with the primary antibody (anti- p-Rb Serine 780) diluted in Superblock followed by secondary antibody (alkaline phosphatase linked anti-rabbit) for a further hour. Plates are developed using the Attophos system and fluorescence read on a Spectramax Gemini plate reader at excitation 450 nm and emission 580 nm. In all cases, IC50 values are calculated from replicate curves, using GraphPad Prism software.
Cell Research:[2]
- Collapse
  • Cell lines: MM.1S, MM.1R, RPMI8226, U266, RPMI8266, RPMI-Dox40, OPM1 cells, primary MM cells and PBMNCs
  • Concentrations: Dissolved in DMSO at a concentration of 10 mM, final concentrations 0.25-4 μM
  • Incubation Time: 24 or 48 hours
  • Method: Cells are incubated with different concentrations of AT7519 for 24 or 48 hours at 37 °C. Cell viability is assessed by measuring 3-(4,5-dimethylthiazol-2-yl)-2,5 diphenyl tetrasodium bromide (MTT) dye absorbance. DNA synthesis is measured by tritiated thymidine uptake (3H-TdR). Apoptosis is assessed by using Annexin V/PI staining. The percentage of cells undergoing apoptosis is defined as the sum of early apoptosis (Annexin V-positive cells) and late apoptosis (Annexin V-positive and PI-positive cells
    (Only for Reference)
Animal Research:[2]
- Collapse
  • Animal Models: Male SCID mice inoculated subcutaneously with MM.1S cells
  • Dosages: 15 mg/kg/day
  • Administration: Dosed i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 10 mg/mL (26.16 mM)
Water Insoluble
Ethanol 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+2% Tween 80+ddH2O
For best results, use promptly after mixing.
1mg/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 382.24
Formula

C16H17Cl2N5O2

CAS No. 844442-38-2
Storage powder
in solvent
Synonyms N/A
Smiles C1CNCCC1NC(=O)C2=C(C=NN2)NC(=O)C3=C(C=CC=C3Cl)Cl

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
NCT01183949 Completed Drug: AT7519M|Drug: Bortezomib Multiple Myeloma Astex Pharmaceuticals Inc.|Multiple Myeloma Research Consortium November 2010 Phase 1|Phase 2

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

CDK Signaling Pathway Map

CDK Inhibitors with Unique Features

Related CDK Products

Tags: buy AT7519 | AT7519 supplier | purchase AT7519 | AT7519 cost | AT7519 manufacturer | order AT7519 | AT7519 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID