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70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  NVj0c3BsTnWwY4Tpc44hSXO|YYm= MojVNUDPxE1? NF\YeXMzPCCq MW\pcoNz\WG|ZYOgeIhmKGGkdX7kZY5k\SCxZjDISXI{KGGwZDDpcoR2[2W|IITo[UBxcG:|cHjvdplt[XSrb36gLIFkfGm4YYTpc44qKG:oIHLveIghTUeIUjDhcoQhUEWUMx?= M2DFV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[3N|c3Lz5{NE[2O|M4PjxxYU6=
MDA-MB-468  M{nDT2Z2dmO2aX;uJGF{e2G7 NEDU[XMyKM7:TR?= MkTjNlQhcA>? M3vBU4lv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGhGWjN? MVm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDZ4N{O3Okc,OjR4NkezO|Y9N2F-
HCC70  M1q5dWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1S2W|Eh|ryP NYHjNVhnPSCm NEC2bHVmdmijbnPld{B1cGViYX70bZBzd2yrZnXyZZRqfmVicnXzdI9ve2V? NWOzTndpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2Olc{PzZpPkK0OlY4Ozd4PD;hQi=>
MDA-MB-468  MmnZS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? M3TaNVEh|ryP MY[1JIQ> MnTx[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKHKnc4DvcpNm NXS5XnAxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS2Olc{PzZpPkK0OlY4Ozd4PD;hQi=>
PC-3 M{PnZWZ2dmO2aX;uJGF{e2G7 M4HjeVAvODB|OD2yMlUh|ryP MnKzNUBp MVPEUXNQ NUTiZlI3cW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ NEPkeWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O|U3Oyd-MkOyPFc2PjN:L3G+
BT474M1 MkL6SpVv[3Srb36gRZN{[Xl? NGL3cYwxNjByM{itNk42KM7:TR?= MVyxJIg> NVzjc4ZKTE2VTx?= NWLLZWdqcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ NF\jWZY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O|U3Oyd-MkOyPFc2PjN:L3G+
IGROV-1 NXLxdog2TnWwY4Tpc44hSXO|YYm= NXLWWVgzOC5yMEO4MVIvPSEQvF2= NFvJcJMyKGh? M2X0UWROW09? MV\pcoR2[2W|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCkb4ToJHRpejNyONMgLHQ{ODhrIHHu[EBU\XJ2N{O= MmHCQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
PC-3 MlXVS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? MYOxM|UwOTBizszN NUn0fYlLOjRxNEivO|IhcA>? MmrYSG1UVw>? NYnXUW0x\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= MorvQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
MCF7-neo/HER2 MUnHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NVPDTYRIOS93L{GwJO69VQ>? M3q1dVI1NzR6L{eyJIg> NYezNZBITE2VTx?= M{\ieoRwe2VvZHXw[Y5l\W62bImgbY5kemWjc3XzJJRp\SCJMPMAl2cyyqCyaHHz[UBxd3C3bHH0bY9vyqB? NF20Wos9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O|U3Oyd-MkOyPFc2PjN:L3G+
BT474M1 M2rxdmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 M1\2W|EwPS9zMDFOwG0> NV3KdnNUOjRxNEivO|IhcA>? NUjEO3BbTE2VTx?= MYrkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
PC-3 MVPBdI9xfG:|aYOgRZN{[Xl? NWG4[2kxOS93L{GwJO69VQ>? NX[3RVJ7OTVxNEivO|IhcA>? M2i0c2ROW09? Ml\0Z4F2e2W|IHGg[I9{\S1iYX7kJJRqdWVvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJIFxd3C2b4TpZ{BidmRibnXjdo91cWNicH;weYxifGmxboO= MXK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
MCF7-neo/HER2 NHvjSlhCeG:ydH;zbZMhSXO|YYm= NU\mZ4UxOS93L{GwJO69VQ>? M3jSPVE2NzR6L{eyJIg> NI\JepJFVVOR MXXjZZV{\XNiYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gZZBweHSxdHnjJIFv\CCwZXPyc5Rq[yCyb4D1cIF1cW:wcx?= MmrXQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
BT474M1 NWTLXm1oSXCxcITvd4l{KEG|c3H5 NVXUSJJHOS93L{GwJO69VQ>? M1ywVVE2NzR6L{eyJIg> MXzEUXNQ NVvSRnNR[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MmP0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
LNCAP MXzDfZRwfG:6aXPpeJkh[XO|YYm= MWC3NkBpenN? NED3XHpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhemW|YYr1dolvKHSxIILld49zfW[rbjDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjB7NTFOwG0v NIXJWlk9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
LNCAP MXfGeY5kfGmxbjDhd5NigQ>? NF;0VJQyNjViaILz M4XwN2lvcGmkaYTpc44hd2ZiQXv0NUBqdiCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDwbI9{eGixconsZZRqd25ib3[gVHJCWzRyIHH0JHRpejJ2NjDh[pRmeiBzLkWgbJJ{NCCLQ{WwJF0hOC5zNUeg{txONg>? M3L1elxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
PC3 MlfrSpVv[3Srb36gZZN{[Xl? MkjUOVAhdWdxa3e= M{\JbFkhcHK| M2frRnBt[XOvYTDjc45k\W62cnH0bY9vKGmwIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iUFOzJINmdGy|IHH0JFUxKG2pL3vnMEBxdyCjdDC5JIhzeyCkeTDMR{9OWy:PUzDhcoFtgXOrczygR5AhRSByLkWg{txONg>? M{fJS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
BT474M1 MVTDfZRwfG:6aXPpeJkh[XO|YYm= MljoPVYhcHK| MWLDfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDCWFQ4PE1zIHPlcIx{KGG|c3Xzd4VlKGG|IHTlZ5Jm[XOnIHnuJINmdGxidnnhZoltcXS7IHHmeIVzKDl4IHjyd{BjgSCFZXzsWIl1emVvR3zvJIF{e2G7LDDJR|UxKD1iMTFOwG0v MnOyQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O|UoRjJ{OUO0OVc2RC:jPh?=
PC3 NUHHUI1LS3m2b4TvfIlkcXS7IHHzd4F6 NEfpOGU6PiCqcoO= NGTxVWpEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhQTZiaILzJIJ6KEOnbHzUbZRz\S2JbH:gZZN{[XluIFnDOVAhRSBzIN88UU4> MVu8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
MCF7 Mkm0R5l1d3SxeHnjbZR6KGG|c3H5 NWfRV5dyQTZiaILz MX3DfZRwfG:6aXPpeJkh[WejaX7zeEBpfW2jbjDNR2Y4KGOnbHzzJI93\XKneIDy[ZN{cW6pIFjldlIh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6gZ4VtdCC4aXHibYxqfHliYX\0[ZIhQTZiaILzJIJ6KEOnbHzUbZRz\S2JbH:gZZN{[XluIFnDOVAhRSBzIN88UU4> MlrxQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O|UoRjJ{OUO0OVc2RC:jPh?=
PC3 NWTENnpETnWwY4Tpc44h[XO|YYm= M2jnPVUxKG2pL3vn M4\oclEhcHJ? M1X0SHBt[XOvYTDjc45k\W62cnH0bY9vKGmwIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iUFOzJINmdGy|IHH0JFUxKG2pL3vnMEBxdyCjdDCxJIhzKGK7IFzDM21UN02VIHHuZYx6e2m|LDDDdEA:KDdwNDFOwG0v NXOyPJVjRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3 MUDGeY5kfGmxbjDhd5NigQ>? M2njO|ExOCCvZz;r[y=> MV:4JIhzew>? Mki3TY5pcWKrdHnvckBw\iCDa4SgbY4hdnVxboWgcY92e2VieHXuc4dz[W[2ZXSge4l1cCCqdX3hckBRSzNiY3XscJMh[XO|ZYPz[YQh[XNiZHXjdoVie2ViaX6geJVud3JicD3TOnJRKGyndnXsJIF1KDFyMDDt[{9s\yxicH:gZZQhQCCqcoOgZpkhTUyLU1GgdoVt[XSrdnWgeI8hfG:2YXygV|ZTWA>? MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
MCF7 M4TFeGZ2dmO2aX;uJIF{e2G7 Mo\VTY5pcWKrdHnvckBw\iCDa4SxMY1m\GmjdHXkJHBTSVN2MDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iTVPGO{Bk\WyuczDveoVz\XiycnXzd4lv\yCKZYKy NI\MZW89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
BT474M1 NGHVUJJHfW6ldHnvckBie3OjeR?= MXjJcohq[mm2aX;uJI9nKEGtdEGtcYVlcWG2ZXSgVHJCWzRyIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCEVES3OG0yKGOnbHzz M1HOOVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
PC3 NHXmWIRHfW6ldHnvckBie3OjeR?= MlXvTY5pcWKrdHnvckBw\iCDa4SxMY1m\GmjdHXkJHBTSVN2MDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iUFOzJINmdGy| MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
LNCAP NWqxNYgxTnWwY4Tpc44h[XO|YYm= NH7s[Y9KdmirYnn0bY9vKG:oIFHreFEudWWmaXH0[YQhWFKDU{SwJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDMUmNCWCClZXzsdy=> Mn73QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O|UoRjJ{OUO0OVc2RC:jPh?=
A673 NH7neGhyUFSVIHHzd4F6 NXrEXI9UeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= NHz2ToE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
DAOY NVXnRWxqeUiWUzDhd5NigQ>? MWjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? NInG[GU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 M4roRZFJXFNiYYPzZZk> MnnOdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NGPJWlE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 MXHxTHRUKGG|c3H5 MkfldWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| M2X4S|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD M3TUdJFJXFNiYYPzZZk> MUTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM> MXm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-SH M3;aWpFJXFNiYYPzZZk> MkHDdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= MlX0QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
BT-12 MVHxTHRUKGG|c3H5 MXnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvMUKgZ4VtdHN? NXHGO|QyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
MG 63 (6-TG R) NGHXT5RyUFSVIHHzd4F6 NG\lWmpyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTVegOlMhMDZvVFegVkkh[2WubIO= NHzQNXM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 MWrxTHRUKGG|c3H5 MmTidWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE6EMU[0N{Bk\Wyucx?= NWfITHpuRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 MV3xTHRUKGG|c3H5 MlHPdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKE:KUz21NEBk\Wyucx?= M3\6RlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
LAN-5 NUfMTlRueUiWUzDhd5NigQ>? MUXxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> NUfD[ZZsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-SH M3W3fpFJXFNiYYPzZZk> M4XzeZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vU1igZ4VtdHN? NWTXeHRFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh41 M4LMS5FJXFNiYYPzZZk> M13zdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCUaESxJINmdGy| MmTPQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
MG 63 (6-TG R) NWLmbWNYeUiWUzDhd5NigQ>? MlnodWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgUWchPjNiKE[tWGchWiliY3XscJM> M1\NS|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh30 M1W3U5FJXFNiYYPzZZk> M{nLXZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOzBiY3XscJM> MmnlQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
Rh41 M{nC[pFJXFNiYYPzZZk> Mly2dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohS2:wZnnycYF1d3K7IIPjdoVmdiCob4KgVog1OSClZXzsdy=> NXnrd5pkRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MkLEdWhVWyCjc4PhfS=> MYfxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW0pvR1LNNkBk\Wyucx?= MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
SK-N-MC NVi5ZpFYeUiWUzDhd5NigQ>? NH3hfmFyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiU1utUk1OSyClZXzsdy=> Mme2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
NB-EBc1 NUXOSohKeUiWUzDhd5NigQ>? NV;4XoNIeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CMWVD[zFiY3XscJM> MYq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
LAN-5 MU\xTHRUKGG|c3H5 M{O5[5FJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCOQV6tOUBk\Wyucx?= NYL6fm1SRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Rh18 NUPY[lZEeUiWUzDhd5NigQ>? NW\RfIxVeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoNVgh[2WubIO= M1rkflxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
SK-N-MC M4PQfZFJXFNiYYPzZZk> M2\IOJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHNMNU5vTVOgZ4VtdHN? MoTYQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
TC32 NFrZcpFyUFSVIHHzd4F6 NEXVe49yUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBVSzN{IHPlcIx{ MYW8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 M17XWJFJXFNiYYPzZZk> NUHNXZUxeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
PUMA ; 

PubMed: 30185800     


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

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. 

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. 

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.

30185800 26469692
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
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、MSDS / 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、MSDS / 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

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

Akt Signaling Pathway Map

Akt Inhibitors with Unique Features

相关Akt产品

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID