Ipatasertib (GDC-0068)

For research use only. Not for use in humans.

目录号：S2808 别名： RG7440

Ipatasertib (GDC-0068) Chemical Structure

CAS No. 1001264-89-6

Ipatasertib (GDC-0068, RG7440)是一种高选择性的pan-Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为5 nM/18 nM/8 nM，比作用于PKA选择性高620倍。Phase 2。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3094.44 现货
RMB 2192.93 现货
RMB 3025.41 现货
RMB 6626.67 现货
RMB 8763.3 现货
RMB 13677.3 现货
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客户使用Selleck生产的Ipatasertib (GDC-0068)发表文献93篇：

产品安全说明书

Akt抑制剂选择性比较

生物活性

产品描述 Ipatasertib (GDC-0068, RG7440)是一种高选择性的pan-Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为5 nM/18 nM/8 nM，比作用于PKA选择性高620倍。Phase 2。
靶点
Akt1 [1]
(Cell-free assay)		 Akt3 [1]
(Cell-free assay)		 Akt2 [1]
(Cell-free assay)
5 nM 8 nM 18 nM
体外研究

对一大组230种激酶测试，GDC-0068只抑制3种激酶，浓度为 1 μM 时抑制70%以上,(抑制PRKG1α,PRKG1β,和p70S6K时, IC50分别为98 nM, 69 nM, 和 860 nM)。GDC-0068 作用于Akt比作用于PKA 选择性高100倍以上，抑制Akt时 IC50为3.1 μM。GDC-0068处理LNCaP, PC3 和 BT474M1 细胞,抑制Akt底物PRAS40磷酸化,IC50分别为157 nM, 197 nM, 和208 nM。而且, GDC-0068选择性抑制细胞周期进展和Akt信号驱动的癌细胞活力, 包括肿瘤抑制基因PTEN缺陷,PIK3CA致癌基因突变, 和HER2扩增,在HER2+和Luminal 亚型中作用效果最强。[1-4]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC70  MVTGeY5kfGmxbjDBd5NigQ>? M2Hn[VEh|ryP MYmyOEBp MUnpcoNz\WG|ZYOgeIhmKGGkdX7kZY5k\SCxZjDISXI{KGGwZDDpcoR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gLIFkfGm4YYTpc44qKG:oIHLveIghTUeIUjDhcoQhUEWUMx?= NFXVPIU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O|M4Pid-MkS2Olc{PzZ:L3G+
MDA-MB-468  NY\lTWo6TnWwY4Tpc44hSXO|YYm= MmrjNUDPxE1? NUn3Z2ZzOjRiaB?= M1\DW4lv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGhGWjN? NF\VdW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O|M4Pid-MkS2Olc{PzZ:L3G+
HCC70  NFXUWHBIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MlTnNUDPxE1? M1jE[|Uh\A>? MWflcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUhemW|cH;ud4U> NWjodZRVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2Olc{PzZpPkK0OlY4Ozd4PD;hQi=>
MDA-MB-468  MYTHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? M1mx[|Eh|ryP MXq1JIQ> NHvFVY1mdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmVicnXzdI9ve2V? MorJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkezO|YoRjJ2Nk[3N|c3RC:jPh?=
PC-3 MnPSSpVv[3Srb36gRZN{[Xl? MUmwMlAxOzhvMj61JO69VQ>? M1i0[VEhcA>? MXvEUXNQ NH3kdo1qdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> NWjOd5doRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
BT474M1 NWPBRVVWTnWwY4Tpc44hSXO|YYm= MXewMlAxOzhvMj61JO69VQ>? NYnacWFXOSCq MmTHSG1UVw>? NIrkfWlqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> MXS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
IGROV-1 MYfGeY5kfGmxbjDBd5NigQ>? NVfmR2xtOC5yMEO4MVIvPSEQvF2= NWPvXYtUOSCq M1XNN2ROW09? M1XZWolv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> M3ftXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Mki3OVY{Lz5{M{K4O|U3OzxxYU6=
PC-3 MoHwS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NV3zbVNMOS93L{GwJO69VQ>? NU\0fHZuOjRxNEivO|IhcA>? M4\hZWROW09? M3vJdYRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NYG1[FdORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
MCF7-neo/HER2 MXzHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MnvSNU82NzFyIN88US=> MUKyOE81QC95MjDo NWD4N5dCTE2VTx?= M{O2NIRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NY\oW|hqRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
BT474M1 NUnlZ|RiT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= MlHvNU82NzFyIN88US=> MnntNlQwPDhxN{KgbC=> MmTWSG1UVw>? MVzkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh NYLmVm5PRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
PC-3 MkPaRZBweHSxc3nzJGF{e2G7 NITRb2kyNzVxMUCg{txO M2flS|E2NzR6L{eyJIg> MUHEUXNQ M13Hc4NifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z MUS8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
MCF7-neo/HER2 NXvCTG11SXCxcITvd4l{KEG|c3H5 MUixM|UwOTBizszN MkKwNVUwPDhxN{KgbC=> NUfnUWkzTE2VTx?= NGraToFk[XW|ZYOgZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4h[XCxcITveIlkKGGwZDDu[YNzd3SrYzDwc5B2dGG2aX;udy=> NWK0TZNPRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
BT474M1 NETjSmJCeG:ydH;zbZMhSXO|YYm= M1Ozc|EwPS9zMDFOwG0> MmDFNVUwPDhxN{KgbC=> MkjJSG1UVw>? NIHleIZk[XW|ZYOgZUBld3OnLTDhcoQhfGmvZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4h[XCxcITveIlkKGGwZDDu[YNzd3SrYzDwc5B2dGG2aX;udy=> MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
LNCAP NHyxdYxEgXSxdH;4bYNqfHliYYPzZZk> Mli3O|IhcHK| NFvvN5REgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhemW|YYr1dolvKHSxIILld49zfW[rbjDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjB7NTFOwG0v NIrDU2I9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
LNCAP MnG2SpVv[3Srb36gZZN{[Xl? MoO1NU42KGi{cx?= NXy4XGtZUW6qaXLpeIlwdiCxZjDBb5QyKGmwIHj1cYFvKEyQQ1HQJINmdGy|IHHzd4V{e2WmIHHzJJBpd3OyaH;yfYxifGmxbjDv[kBRWkGVNECgZZQhXGi{MkS2JIFnfGW{IEGuOUBpenNuIFnDOVAhRSByLkG1O{DPxE1w MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
PC3 MmLMSpVv[3Srb36gZZN{[Xl? NVnYVY9EPTBibXevb4c> MoLEPUBpenN? M2r4SXBt[XOvYTDjc45k\W62cnH0bY9vKGmwIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iUFOzJINmdGy|IHH0JFUxKG2pL3vnMEBxdyCjdDC5JIhzeyCkeTDMR{9OWy:PUzDhcoFtgXOrczygR5AhRSByLkWg{txONg>? NXi0bHV2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
BT474M1 MY\DfZRwfG:6aXPpeJkh[XO|YYm= MYW5OkBpenN? MonNR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gRnQ1PzSPMTDj[YxteyCjc4Pld5Nm\CCjczDk[YNz\WG|ZTDpckBk\WyuII\pZYJqdGm2eTDh[pRmeiB7NjDodpMh[nliQ3XscHRqfHKnLVfsc{Bie3OjeTygTWM2OCB;IEGg{txONg>? NIrwc5g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
PC3 M{DJZmN6fG:2b4jpZ4l1gSCjc4PhfS=> NIXBT4k6PiCqcoO= M4DFOGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA6PiCqcoOgZpkhS2WubGTpeJJmNUeubzDhd5NigSxiSVO1NEA:KDFizszNMi=> M4T6[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
MCF7 NXPEb2xYS3m2b4TvfIlkcXS7IHHzd4F6 M2SyeVk3KGi{cx?= NVTXPJdQS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCxdnXy[ZhxemW|c3nu[{BJ\XJ{IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEm2JIhzeyCkeTDD[YxtXGm2cnWtS4xwKGG|c3H5MEBKSzVyIE2gNUDPxE1w MYK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
PC3 MVHGeY5kfGmxbjDhd5NigQ>? NHz5O5c2OCCvZz;r[y=> NYTYZ3o4OSCqch?= NV3i[mJNWGyjc33hJINwdmOnboTyZZRqd25iaX6gcpUwdnVibX;1d4UhgGWwb3fyZYZ1\WRid3n0bEBpfW2jbjDQR|Mh[2WubIOgZZQhPTBibXevb4ctKHCxIHH0JFEhcHJiYomgUGMwVVNxTWOgZY5idHm|aYOsJGNxKD1iNz60JO69VS5? M3vTV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
PC3 M4jaW2Z2dmO2aX;uJIF{e2G7 MoX0NVAxKG2pL3vn NWLr[2ptQCCqcoO= MY\Jcohq[mm2aX;uJI9nKEGtdDDpckBvfS:wdTDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjD0eY1weiCyLWO2VnAhdGW4ZXygZZQhOTByIH3nM4toNCCybzDheEA5KGi{czDifUBGVEmVQTDy[YxifGm4ZTD0c{B1d3SjbDDTOnJR MXG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
MCF7 NFXtXVVHfW6ldHnvckBie3OjeR?= MmD0TY5pcWKrdHnvckBw\iCDa4SxMY1m\GmjdHXkJHBTSVN2MDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVPGO{Bk\WyuczDveoVz\XiycnXzd4lv\yCKZYKy M1P1eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
BT474M1 NI\LO|ZHfW6ldHnvckBie3OjeR?= MlTkTY5pcWKrdHnvckBw\iCDa4SxMY1m\GmjdHXkJHBTSVN2MDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQmS0O|ROOSClZXzsdy=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
PC3 MV\GeY5kfGmxbjDhd5NigQ>? MXPJcohq[mm2aX;uJI9nKEGtdEGtcYVlcWG2ZXSgVHJCWzRyIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCSQ{OgZ4VtdHN? MYi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
LNCAP MXvGeY5kfGmxbjDhd5NigQ>? MXjJcohq[mm2aX;uJI9nKEGtdEGtcYVlcWG2ZXSgVHJCWzRyIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCOTlPBVEBk\Wyucx?= NXLJdXBiRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
A673 M{GzRZFJXFNiYYPzZZk> M4DCNpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCDNkezJINmdGy| M3e1e|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY M4m4cZFJXFNiYYPzZZk> M1;UVJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCGQV;ZJINmdGy| MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NVXwSGRFeUiWUzDhd5NigQ>? MWnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
BT-37 MVHxTHRUKGG|c3H5 MYXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN? NYP2XWM3RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
RD M3z1cpFJXFNiYYPzZZk> NXi1Sox4eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLEJINmdGy| NXTMdpNKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH NX7mOYVWeUiWUzDhd5NigQ>? M1zBTJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz NHvieZA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-12 MVrxTHRUKGG|c3H5 M1fSU5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCEVD2xNkBk\Wyucx?= Ml7RQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) M{HnbZFJXFNiYYPzZZk> NUG3cINSeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz M4rmXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB1643 NHe1So1yUFSVIHHzd4F6 NYTFW4hZeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> MVq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
OHS-50 MUPxTHRUKGG|c3H5 MmThdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= NV\aWHVvRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 NYO2SW9KeUiWUzDhd5NigQ>? MXPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> MkTXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-SH M1z5WZFJXFNiYYPzZZk> MmjkdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgV2suVi2VSDDj[Yxtew>? NYfrSIZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 MWfxTHRUKGG|c3H5 MW\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmh2MTDj[Yxtew>? M{XkOlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M1\xbJFJXFNiYYPzZZk> MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDNS{A3OyBqNj3US{BTMSClZXzsdy=> NFfSe409[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh30 NFOxTXByUFSVIHHzd4F6 MWPxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDSbFMxKGOnbHzz NGrWbZU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh41 Mmn0dWhVWyCjc4PhfS=> NHKw[4pyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{ M{nVUVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SJ-GBM2 M1G0eJFJXFNiYYPzZZk> NYXrRoR{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGPKMWdDVTJiY3XscJM> NUTsd3FwRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC MoLadWhVWyCjc4PhfS=> Mm\0dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
NB-EBc1 MWPxTHRUKGG|c3H5 M{C1bZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCQQj3FRoMyKGOnbHzz NYW1XW5QRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MlGxdWhVWyCjc4PhfS=> MWfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVEGQLUWgZ4VtdHN? NFvUfnQ9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Rh18 MoTLdWhVWyCjc4PhfS=> MnnHdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKqMUigZ4VtdHN? MVy8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC M2fZU5FJXFNiYYPzZZk> M3XEZ5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? NFWwNng9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
TC32 NH7kZnNyUFSVIHHzd4F6 MnLldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgWGM{OiClZXzsdy=> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 Mn\rdWhVWyCjc4PhfS=> MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> M3LxSVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=

... Click to View More Cell Line Experimental Data
Assay
Methods Test Index PMID
Western blot
p-PRAS40(T246) / PRAS40 / p-ERK / ERK / pFOXO1 / pFOXO3a / pGSK3b(S9) / pAS160(S318) / pBAD(S136) / pS6 / p4E-BP1; 

PubMed: 26469692     


MDA-MB 453 breast cancer cell line (PIK3CAH1047R; Her2 amp) were treated with various concentrations (1 = 0, 2 = 0.012, 3 = 0.037, 4 = 0.11, 5 = 0.33, and 6 = 1 μM) of ARQ 092, ARQ 751, MK-2206 or GDC-0068 for 2 hours. pAKT(S473), pAKT(T308), pPRAS40(T246), pFOXO1(T24) /3a(T36), pGSK3β(S9), pAS160(S318), pBAD(S136), pS6(S235/236) and p4E-BP1(S65) and phospho ERK were assessed by western blot analysis.

cleaved-caspase3; 

PubMed: 30185800     


(a, c, e) Western blotting analysis of PUMA and C-Caspase3 expression after the treatment of 10 μM ipatasertib in combination with (a) 20 mg/ml 5-FU or (c) 40 μM Cisplatin or (e) 20 mM Regorafenib alone, or their combinations for 24 h in HCT116. 

Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1; 

PubMed: 30185800     


Noxa, Bid, Bad, Bim, Bcl-2, Bcl-XL, Mcl-1 were detected in HCT-116 cells after ipatasertib for 24 h. 

p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 ; 

PubMed: 30185800     


The expressions of P-Akt (S473), P-FoxO3a (S253), P-p65(S536), and PUMA were detected after the treatment of 10 μM ipatasertib in HCT116 at 0, 6, 12, and 24 h after 10 μM ipatasertib treatment. 

PUMA ; 

PubMed: 30185800     


Western blotting analysis of PUMA expression in various colon cancer cell lines treated with 10 μM ipatasertib for 24 h.

26469692 30185800
体内研究 GDC-0068口服处理给药PC3前列腺移植瘤模型，诱导p-PRAS40下调。GDC-0068 处理BT474-Tr移植瘤,降低 pS6 和 peIF4G 水平,重新定位FOXO3a到细胞核,且诱导 HER3 和pERK的反馈上调。GDC-0068 处理多种移植瘤模型，具有有效抗癌活性，包括PTEN-缺陷的前列腺癌模型LNCaP 和 PC3, PIK3CA H1047R 突变的乳腺癌模型 KPL-4, 和 MCF7-neo/HER2肿瘤模型。[1-4]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验：[1]
- 合并
  • Animal Models: 携带LNCaP, PC3, KPL-4, 或MCF7移植瘤的雌性裸鼠
  • Dosages: ~100 mg/kg/day
  • Administration: 口服处理
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 92 mg/mL (200.87 mM)
Water Insoluble
Ethanol '92 mg/mL

* 溶解度检测是由Selleck技术部门检测的，可能会和文献中提供的溶解度有所差异，这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 458
化学式

C24H32ClN5O2
CAS号 1001264-89-6
储存条件 粉状
溶于溶剂
别名 RG7440

动物体内配方计算器 (澄清溶液)

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量 只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液，使用的计算公式为：

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时，请务必参考Selleck产品标签上、SDS / COA（可在Selleck的产品页面获得）批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • 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):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量：

总分子量：g/mol

注：化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01090960 Completed Drug: GDC-0068 Solid Cancers Genentech Inc. March 2010 Phase 1

技术支持

在订购、运输、储存和使用我们的产品的任何阶段，您遇到的任何问题，均可以通过拨打我们的热线电话400-668-6834，或者技术支持邮箱tech@selleck.cn，直接联系到我们。我们会在24小时内尽快联系您。

操作手册

如果有其他问题，请给我们留言。

  • * 必填项
Selleck产品目录册

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

  • 选择性强的Akt抑制剂

    CCT128930 : Akt2-selective, IC50=6 nM.

  • 活性最高的Akt抑制剂

    AZD5363 : Akt1, IC50=3 nM; Akt2, IC50=8 nM; Akt3, IC50=8 nM.

  • 用于临床的Akt抑制剂

    Perifosine (KRX-0401) : Phase III for relapsed and refractory multiple myeloma.

  • 最新的Akt抑制剂

    AZD5363 : Potent inhibitor of all isoforms of Akt (Akt1/Akt2/Akt3) with IC50 of 3 nM/8 nM/8 nM, similar to P70S6K/PKA and lower activity towards ROCK1/2.

相关Akt产品

  • Afuresertib (GSK2110183) New

    Afuresertib (GSK2110183)是一种有效的，口服生物可利用的 Akt 抑制剂，对Akt1，Akt2，和 Akt3 的 Ki 分别为 0.08 nM，2 nM，和 2.6 nM。Phase 2。

  • AT13148 New

    AT13148是一种口服的，ATP竞争性的，多AGC kinase抑制剂，对Akt1/2/3，p70S6K，PKA，和ROCKI/II的IC50分别为38 nM/402 nM/50 nM，8 nM，3 nM，和6 nM/4 nM。Phase 1。

  • SC79 New

    SC79是一种大脑渗透性Akt磷酸化激活剂，也是一种Akt-PH域易位抑制剂。

  • MK-2206 2HCl

    MK-2206 2HCl是一种高度选择性的Akt1/2/3抑制剂，在无细胞试验中IC50分别为8 nM/12 nM/65 nM；对250种其他蛋白激酶没有抑制活性。MK-2206 2HCl 在肿瘤细胞中可诱导自噬和凋亡。Phase 2。

    Features:MK-2206是第一个进入临床研究阶段的Akt小分子变构抑制剂。

  • Capivasertib (AZD5363)

    Capivasertib (AZD5363)有效抑制Akt(Akt1/Akt2/3)的所有亚型，在无细胞试验中IC50为3 nM/8 nM/8 nM，对P70S6K/PKA也具有相似的抑制效果，而对ROCK1/2抑制活性较低。Phase 2。

    Features:AZD5363具有良好的临床前期耐受性，和AKT抑制剂的药效学特性，且不同于其他AKT抑制剂具有卓越的特性，已经进入临床开发阶段。[2]

  • GSK690693

    GSK690693 是一种泛Akt抑制剂，靶向作用于Akt1/2/3，在无细胞试验中IC50为2 nM/13 nM/9 nM，也对AGC激酶家族:PKA，PrkX和PKC同工酶敏感。GSK690693 也能有效地抑制CAMK家族的 AMPK 和 DAPK3，对应的IC50值分别为50 nM和81 nM。GSK690693 可影响 Unc-51-like autophagy activating kinase 1 (ULK1) 的活性并有效地抑制 STING-dependent IRF3 的激活。Phase 1。

  • Perifosine (KRX-0401)

    Perifosine (KRX-0401, NSC639966, D21266)是一种新型的Akt抑制剂，在MM.1S细胞中IC50为4.7 μM，靶向作用于Akt的pleckstrin同源结构域。Phase 3。

  • Triciribine (NSC 154020)

    Triciribine (NSC 154020, VD-0002, vqd-002, API-2, TCN) 是一种DNA synthesis抑制剂，也抑制PC3细胞系中的Akt和CEM-SS，H9，H9IIIB，U1细胞中的HIV-1，IC50分别为130 nM和20 nM；对PI3K/PDK1没有抑制作用；作用于缺乏腺苷激酶的细胞，活性降低5000倍。Phase 1/2。

  • Honokiol (NSC 293100)

    Honokiol (NSC 293100)是木兰的有效成分，抑制Akt磷酸化，且促进ERK1/2磷酸化。Honokiol 可造成 G0/G1 期阻滞，并可通过 ROS/ERK1/2 信号通路来诱导凋亡和自噬。Honokiol 可抑制 hepatitis C virus (HCV) 感染。Phase 3。

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID