Ipatasertib (GDC-0068)

For research use only.

Catalog No.S2808 Synonyms: RG7440

81 publications

Ipatasertib (GDC-0068) Chemical Structure

CAS No. 1001264-89-6

Ipatasertib (GDC-0068, RG7440) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

Selleck's Ipatasertib (GDC-0068) has been cited by 81 publications

Purity & Quality Control

Choose Selective Akt Inhibitors

Biological Activity

Description Ipatasertib (GDC-0068, RG7440) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.
Targets
Akt1 [1]
(Cell-free assay)
Akt3 [1]
(Cell-free assay)
Akt2 [1]
(Cell-free assay)
5 nM 8 nM 18 nM
In vitro

Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3 kinases by >70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K, with IC50 of 98 nM, 69 nM, and 860 nM, respectively). GDC-0068 displays >100-fold selectivity for Akt over PKA with IC50 of 3.1 μM. In LNCaP, PC3 and BT474M1 cells, GDC-0068 treatment inhibits the phosphorylation of the Akt substrate, PRAS40 with IC50 of 157 nM, 197 nM, and 208 nM, respectively. Furthermore, GDC-0068 selectively inhibits cell cycle progression and viability of cancer cell lines driven by Akt signaling, including those with defects in the tumor suppressor PTEN, oncogenic mutations in PIK3CA, and amplification of HER2, with strongest effects in HER2+ and Luminal subtypes. [1-4]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC70  NUXLW5NFTnWwY4Tpc44hSXO|YYm= NXjpN41NOSEQvF2= NXPuUmR1OjRiaB?= MlnGbY5kemWjc3XzJJRp\SCjYoXu[IFv[2Vib3[gTGVTOyCjbnSgbY5lfWOnczD0bIUheGixc4Doc5J6dGG2aX;uJEhi[3SrdnH0bY9vMSCxZjDic5RpKEWJRmKgZY5lKEiHUkO= NEDpOYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O|M4Pid-MkS2Olc{PzZ:L3G+
MDA-MB-468  MUjGeY5kfGmxbjDBd5NigQ>? M2TUNlEh|ryP MV2yOEBp MkfibY5kemWjc3XzJJRp\SCjYoXu[IFv[2Vib3[gTGVTOw>? MlewQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkezO|YoRjJ2Nk[3N|c3RC:jPh?=
HCC70  MkLxS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NHyyXngyKM7:TR?= MnnvOUBl MWHlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUhemW|cH;ud4U> MnXzQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkezO|YoRjJ2Nk[3N|c3RC:jPh?=
MDA-MB-468  NWr6Xm53T3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NHzhZpcyKM7:TR?= M{fiWFUh\A>? M13Qc4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>? NF\HVXo9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O|M4Pid-MkS2Olc{PzZ:L3G+
PC-3 NWPvTocxTnWwY4Tpc44hSXO|YYm= NIXOWIYxNjByM{itNk42KM7:TR?= M4rORVEhcA>? NIPVcmRFVVOR M4HPdYlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=> M1KyeFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Mki3OVY{Lz5{M{K4O|U3OzxxYU6=
BT474M1 NF;XUXFHfW6ldHnvckBCe3OjeR?= MlP3NE4xODN6LUKuOUDPxE1? NW\oO4RkOSCq MlfkSG1UVw>? NYLXd|BVcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ M3;tPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ|Mki3OVY{Lz5{M{K4O|U3OzxxYU6=
IGROV-1 M{TUXmZ2dmO2aX;uJGF{e2G7 NH3zVGYxNjByM{itNk42KM7:TR?= NGC5OVcyKGh? MUPEUXNQ NYfRWlhQcW6mdXPld{BiKGSxc3Wt[IVx\W6mZX70JIlv[3KnYYPlJIlvKEGtdDDwbI9{eGixconsZZRqd25iYYSgZo91cCCWaIKzNFjDqCiWM{C4LUBidmRiU3XyOFc{ NFzqU4s9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O|U3Oyd-MkOyPFc2PjN:L3G+
PC-3 MVfHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NWTlVoRROS93L{GwJO69VQ>? NYPme49QOjRxNEivO|IhcA>? NV2wfGdpTE2VTx?= NWrJem9I\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= MmDJQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
MCF7-neo/HER2 MXLHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? MmPxNU82NzFyIN88US=> NFXydJkzPC92OD:3NkBp MUXEUXNQ MV;kc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh NIOxXHM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O|U3Oyd-MkOyPFc2PjN:L3G+
BT474M1 MVXHdo94fGhiSX7obYJqfGmxbjDBd5NigQ>? NUDXWFRzOS93L{GwJO69VQ>? MXmyOE81QC95MjDo NFzJd|FFVVOR MUjkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh MlfhQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ|Mki3OVY{RC:jPh?=
PC-3 NEfGT21CeG:ydH;zbZMhSXO|YYm= M2LQclEwPS9zMDFOwG0> MYKxOU81QC95MjDo NVKxVXIyTE2VTx?= NVXTcWU4[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MV28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
MCF7-neo/HER2 MULBdI9xfG:|aYOgRZN{[Xl? MortNU82NzFyIN88US=> M2\2[FE2NzR6L{eyJIg> NXLZR4ppTE2VTx?= M2WwTINifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z NV;BWphNRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ|PD;hQi=>
BT474M1 NYTY[mFvSXCxcITvd4l{KEG|c3H5 NV\wN4RCOS93L{GwJO69VQ>? M2S0e|E2NzR6L{eyJIg> MXHEUXNQ M1n1[oNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOzJ6N{W2N{c,OjN{OEe1OlM9N2F-
LNCAP NX7qW5o2S3m2b4TvfIlkcXS7IHHzd4F6 NVv6WZpLPzJiaILz MofaR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gUG5ESVBiY3XscJMh[XO|ZYPz[YQh[XNicnXkeYN1cW:wIH;mJJJme2G8dYLpckB1dyC{ZYPvdpVncW5iYX\0[ZIhPzJiaILzMEBKSzVyIE2gNE4xQTVizszNMi=> Mki2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O|UoRjJ{OUO0OVc2RC:jPh?=
LNCAP NWH3RmJRTnWwY4Tpc44h[XO|YYm= NFLhd3QyNjViaILz NFy4cplKdmirYnn0bY9vKG:oIFHreFEhcW5iaIXtZY4hVE6FQWCgZ4VtdHNiYYPz[ZN{\WRiYYOgdIhwe3Cqb4L5cIF1cW:wIH;mJHBTSVN2MDDheEBVcHJ{NE[gZYZ1\XJiMT61JIhzeyxiSVO1NEA:KDBwMUW3JO69VS5? NGjEdVY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
PC3 NFrTfFdHfW6ldHnvckBie3OjeR?= MV:1NEBu\y:tZx?= MXm5JIhzew>? MWXQcIF{dWFiY3;uZ4VvfHKjdHnvckBqdiCwdT;ueUBud3W|ZTD4[Y5w\3KjZoTl[EB4cXSqIHj1cYFvKFCFMzDj[YxteyCjdDC1NEBu\y:tZzygdI8h[XRiOTDodpMh[nliTFOvUXMwVVNiYX7hcJl{cXNuIFPwJF0hOC53IN88UU4> NXnJXoR2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
BT474M1 NEjWcVJEgXSxdH;4bYNqfHliYYPzZZk> NVnh[452QTZiaILz NXP6fZh6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hSlR2N{TNNUBk\WyuczDhd5Nme3OnZDDhd{Bl\WO{ZXHz[UBqdiClZXzsJJZq[WKrbHn0fUBi\nSncjC5OkBpenNiYomgR4VtdFSrdILlMWdtdyCjc4PhfUwhUUN3MDC9JFEh|ryPLh?= NUDINnA6RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3 MX7DfZRwfG:6aXPpeJkh[XO|YYm= MlfRPVYhcHK| MnXHR5l1d3SxeHnjbZR6KGGpYXnud5QhcHWvYX6gVGM{KGOnbHzzJIF{e2W|c3XkJIF{KGSnY4LlZZNmKGmwIHPlcIwhfmmjYnnsbZR6KGGodHXyJFk3KGi{czDifUBE\WyuVHn0doUuT2yxIHHzd4F6NCCLQ{WwJF0hOSEQvF2u M1z5VVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
MCF7 MoPER5l1d3SxeHnjbZR6KGG|c3H5 MUm5OkBpenN? NYi5cZBTS3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCxdnXy[ZhxemW|c3nu[{BJ\XJ{IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEm2JIhzeyCkeTDD[YxtXGm2cnWtS4xwKGG|c3H5MEBKSzVyIE2gNUDPxE1w Ml;wQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O|UoRjJ{OUO0OVc2RC:jPh?=
PC3 MmXkSpVv[3Srb36gZZN{[Xl? MUS1NEBu\y:tZx?= MUmxJIhz NH\KZZBRdGG|bXGgZ49v[2WwdILheIlwdiCrbjDueU9vfSCvb4Xz[UB5\W6xZ4Lh[pRm\CC5aYToJIh2dWGwIGDDN{Bk\WyuczDheEA2OCCvZz;r[{wheG9iYYSgNUBpeiCkeTDMR{9OWy:PUzDhcoFtgXOrczygR5AhRSB5LkSg{txONg>? NGnPWW49[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N|Q2PzV:L3G+
PC3 NXzBUmx5TnWwY4Tpc44h[XO|YYm= NXLxSHR7OTByIH3nM4to MkGzPEBpenN? MX3Jcohq[mm2aX;uJI9nKEGtdDDpckBvfS:wdTDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjD0eY1weiCyLWO2VnAhdGW4ZXygZZQhOTByIH3nM4toNCCybzDheEA5KGi{czDifUBGVEmVQTDy[YxifGm4ZTD0c{B1d3SjbDDTOnJR M{e0ZVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ{OUO0OVc2Lz5{MkmzOFU4PTxxYU6=
MCF7 MkjrSpVv[3Srb36gZZN{[Xl? NILJcFlKdmirYnn0bY9vKG:oIFHreFEudWWmaXH0[YQhWFKDU{SwJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNR2Y4KGOnbHzzJI93\XKneIDy[ZN{cW6pIFjldlI> MUO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
BT474M1 MXLGeY5kfGmxbjDhd5NigQ>? M{DUZmlvcGmkaYTpc44hd2ZiQXv0NU1u\WSrYYTl[EBRWkGVNECgdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFLUOFc1VTFiY3XscJM> NVvVcINbRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3 MWPGeY5kfGmxbjDhd5NigQ>? NG\ldWpKdmirYnn0bY9vKG:oIFHreFEudWWmaXH0[YQhWFKDU{SwJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDQR|Mh[2WubIO= NV;qWllFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N|Q2PzVpPkKyPVM1PTd3PD;hQi=>
LNCAP NFj3N3lHfW6ldHnvckBie3OjeR?= NY\KZo9qUW6qaXLpeIlwdiCxZjDBb5QyNW2nZHnheIVlKFCUQWO0NEBxcG:|cHjvdplt[XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJM> MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl|NEW3OUc,OjJ7M{S1O|U9N2F-
A673 M17CbpFJXFNiYYPzZZk> NUCwfpZOeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFG2O|Mh[2WubIO= M4GzZ|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY MlqzdWhVWyCjc4PhfS=> MVjxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhTEGRWTDj[Yxtew>? NUnVTlRGRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
Saos-2 NYToZo9VeUiWUzDhd5NigQ>? MnrzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOjb4OtNkBk\Wyucx?= NInlWoY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
BT-37 MlTEdWhVWyCjc4PhfS=> MmHzdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUO3JINmdGy| Ml\2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
RD MU\xTHRUKGG|c3H5 Ml36dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFKGIHPlcIx{ NIqxdYc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH MmjBdWhVWyCjc4PhfS=> MoDWdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tV2gh[2WubIO= NW\pW3lpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12 NGPkXHRyUFSVIHHzd4F6 NWXneFZKeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFLUMVEzKGOnbHzz M13mW|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) MlTDdWhVWyCjc4PhfS=> NX33VY1FeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF3HJFY{KCh4LWTHJHIqKGOnbHzz NUHOeG46RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
NB1643 M1G2N5FJXFNiYYPzZZk> MVnxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhVkJzNkSzJINmdGy| NVLHOox2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
OHS-50 NXHB[GZWeUiWUzDhd5NigQ>? NVvp[4Z3eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF;IV{02OCClZXzsdy=> NXLve2tORGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
LAN-5 MWPxTHRUKGG|c3H5 MYHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDMRW4uPSClZXzsdy=> NG\1Umw9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-SH NWLXPFJ6eUiWUzDhd5NigQ>? MVvxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTT{1PNVOKIHPlcIx{ M13hPFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MlvzdWhVWyCjc4PhfS=> NX7UPFdseUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IGLoOFEh[2WubIO= M{LSelxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
MG 63 (6-TG R) M1jjfZFJXFNiYYPzZZk> M1y0WZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJG1IKDZ|IDi2MXRIKFJrIHPlcIx{ MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Rh30 MWHxTHRUKGG|c3H5 M3nTbpFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHJpOzBiY3XscJM> M3zOXlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh41 MlPndWhVWyCjc4PhfS=> NHK5V|JyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCFb37mbZJu[XSxcomgd4Nz\WWwIH\vdkBTcDRzIHPlcIx{ NVTwPIhzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SJ-GBM2 MUfxTHRUKGG|c3H5 MmS4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFOMLVfCUVIh[2WubIO= NYmyOGVVRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N|UyOzlpPkK5OFM2OTN7PD;hQi=>
SK-N-MC NGLsW2RyUFSVIHHzd4F6 Mm\4dWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= M2rDPVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
NB-EBc1 NF7TR4xyUFSVIHHzd4F6 NIDBTolyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiTlKtSWJkOSClZXzsdy=> NF;NNJU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
LAN-5 MlTudWhVWyCjc4PhfS=> NVXGXYxLeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IFzBUk02KGOnbHzz M3myc|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
Rh18 NHnEPJRyUFSVIHHzd4F6 MY\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWmhzODDj[Yxtew>? NFfrRmY9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
SK-N-MC M{PY[ZFJXFNiYYPzZZk> NYDFWWJNeUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiQ3;u[olzdWG2b4L5JJNkemWnbjDmc5IhW0tvTj3NR{Bk\Wyucx?= NHfQTZc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
TC32 NFr5[JZyUFSVIHHzd4F6 M4[yRZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KEOxbn\pdo1ifG:{eTDzZ5Jm\W5iZn;yJHREOzJiY3XscJM> NF\rRXc9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
Saos-2 MlLYdWhVWyCjc4PhfS=> MWTxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBEd26oaYLtZZRwenlic3Py[YVvKG[xcjDTZY9{NTJiY3XscJM> M4e2WVxiKHSjcnfleF0oZ2KuYX7rK{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
In vivo Oral administration of GDC-0068 in PC3 prostate tumor xenografts model induces down-regulation of p-PRAS40. In BT474-Tr xenografts, GDC-0068 treatment reduces pS6 and peIF4G levels, re-localizes FOXO3a to nucleus, and induces feedback upregulation of HER3 and pERK. Administration of GDC-0068 exhibits potent antitumor efficacy in multiple xenograft tumor models, including the PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. [1-4]

Protocol

Animal Research:[1]
- Collapse
  • Animal Models: Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
  • Dosages: ~100 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (200.87 mM)
Water Insoluble
Ethanol '92 mg/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 458
Formula

C24H32ClN5O2

CAS No. 1001264-89-6
Storage powder
in solvent
Synonyms RG7440
Smiles CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Step 2: Enter the in vivo formulation ()
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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
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*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 )

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* 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):
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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
NCT01090960 Completed Drug: GDC-0068 Solid Cancers Genentech Inc. March 2010 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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID