Name: Ipatasertib (GDC-0068)
Brand: Selleck Chemicals
SKU: S2808
Rating: 5 (87 reviews)

Ipatasertib (GDC-0068) Chemical Structure

CAS No. 1001264-89-6

Selleck's Ipatasertib (GDC-0068) has been cited by 87 publications

Purity & Quality Control

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Akt Signaling Pathway Map

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	NWXGcItwTnWwY4Tpc44hSXO\|YYm=	NHHQ[2MyKM7:TR?=	M2nZV\|I1KGh?		NIfJbI5qdmO{ZXHz[ZMhfGinIHHieY5l[W6lZTDv[kBJTVJ\|IHHu[EBqdmS3Y3XzJJRp\SCyaH;zdIhwenmuYYTpc44hMGGldHn2ZZRqd25rIH;mJIJwfGhiRVfGVkBidmRiSFXSNy=>	NHHPco89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O\|M4Pid-MkS2Olc{PzZ:L3G+
MDA-MB-468	MY\GeY5kfGmxbjDBd5NigQ>?	MlvTNUDPxE1?	M3TwcVI1KGh?		M{PZXYlv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGhGWjN?	M{H2eVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2Nk[3N\|c3Lz5{NE[2O\|M4PjxxYU6=
HCC70	MlvSS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MXexJO69VQ>?	NVzMV2x3PSCm		MWjlcohidmOnczD0bIUh[W62aYDyc4xq\mW{YYTpeoUhemW\|cH;ud4U>	Mkf2QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjR4NkezO\|YoRjJ2Nk[3N\|c3RC:jPh?=
MDA-MB-468	MoHHS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl?	MW[xJO69VQ>?	NV\HRYsxPSCm		M4nTZ4VvcGGwY3XzJJRp\SCjboTpdJJwdGmoZYLheIl3\SC{ZYPwc45{\Q>?	NH6yfI89[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NE[2O\|M4Pid-MkS2Olc{PzZ:L3G+
PC-3	NUD1UXQ{TnWwY4Tpc44hSXO\|YYm=	M{\zXFAvODB\|OD2yMlUh\|ryP	M{nqPVEhcA>?	MWPEUXNQ	MVjpcoR2[2W\|IHGg[I9{\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gRYt1KHCqb4PwbI9zgWyjdHnvckBifCCkb4ToJHRpejNyONMgLHQ{ODhrIHHu[EBU\XJ2N{O=	M4O3[FxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|Mki3OVY{Lz5{M{K4O\|U3OzxxYU6=
BT474M1	NF\BcZpHfW6ldHnvckBCe3OjeR?=	MYewMlAxOzhvMj61JO69VQ>?	MknsNUBp	MmrESG1UVw>?	NGnFcodqdmS3Y3XzJIEh\G:\|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR\|MEipJIFv\CCVZYK0O\|M>	MmTuQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ\|Mki3OVY{RC:jPh?=
IGROV-1	MnvoSpVv[3Srb36gRZN{[Xl?	M4rLOVAvODB\|OD2yMlUh\|ryP	MXKxJIg>	MV7EUXNQ	M2OydIlv\HWlZYOgZUBld3OnLXTldIVv\GWwdDDpcoNz\WG\|ZTDpckBCc3RicHjvd5Bpd3K7bHH0bY9vKGG2IHLveIghXGi{M{C4xsApXDNyODmgZY5lKFOnckS3Ny=>	M13TWFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|Mki3OVY{Lz5{M{K4O\|U3OzxxYU6=
PC-3	NUn1eHN3T3Kxd4ToJGlvcGmkaYTpc44hSXO\|YYm=	M3O3WFEwPS9zMDFOwG0>	NXOxU5ZCOjRxNEivO\|IhcA>?	MUnEUXNQ	MkjH[I9{\S2mZYDlcoRmdnSueTDpcoNz\WG\|ZYOgeIhmKEdy4pETS\|HDqHCqYYPlJJBweHWuYYTpc47DqA>?	NETteIE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{M{K4O\|U3Oyd-MkOyPFc2PjN:L3G+
MCF7-neo/HER2	M2ntRWdzd3e2aDDJcohq[mm2aX;uJGF{e2G7	NHr5fWoyNzVxMUCg{txO	MlfhNlQwPDhxN{KgbC=>	M2nNOWROW09?	NXLTbXpI\G:\|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?=	NVTtR2k4RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ\|PD;hQi=>
BT474M1	M4XGS2dzd3e2aDDJcohq[mm2aX;uJGF{e2G7	MVKxM\|UwOTBizszN	NFr0b2kzPC92OD:3NkBp	Ml7sSG1UVw>?	MkDR[I9{\S2mZYDlcoRmdnSueTDpcoNz\WG\|ZYOgeIhmKEdy4pETS\|HDqHCqYYPlJJBweHWuYYTpc47DqA>?	NUjJd3dzRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkOyPFc2PjNpPkKzNlg4PTZ\|PD;hQi=>
PC-3	MWXBdI9xfG:\|aYOgRZN{[Xl?	NVnvUlJNOS93L{GwJO69VQ>?	NXniZpd5OTVxNEivO\|IhcA>?	NYTVZnVJTE2VTx?=	M1;RVINifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG\|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z	M3;K[VxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|Mki3OVY{Lz5{M{K4O\|U3OzxxYU6=
MCF7-neo/HER2	Mo[1RZBweHSxc3nzJGF{e2G7	MV2xM\|UwOTBizszN	NEHCdJEyPS92OD:3NkBp	MXTEUXNQ	M130[YNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG\|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z	M{fiXFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ\|Mki3OVY{Lz5{M{K4O\|U3OzxxYU6=
BT474M1	NX;UU4pTSXCxcITvd4l{KEG\|c3H5	MUWxM\|UwOTBizszN	MYWxOU81QC95MjDo	M1\6WmROW09?	MUPjZZV{\XNiYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gZZBweHSxdHnjJIFv\CCwZXPyc5Rq[yCyb4D1cIF1cW:wcx?=	Mn;ZQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjN{OEe1OlMoRjJ\|Mki3OVY{RC:jPh?=
LNCAP	NH;qPYREgXSxdH;4bYNqfHliYYPzZZk>		NVLmNWxNPzJiaILz		NFf3[ZlEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBNVkODUDDj[YxteyCjc4Pld5Nm\CCjczDy[YR2[3Srb36gc4YhemW\|YYr1dolvKHSxIILld49zfW[rbjDh[pRmeiB5MjDodpMtKEmFNUCgQUAxNjB7NTFOwG0v	NIq2ZpU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N\|Q2PzV:L3G+
LNCAP	MkCySpVv[3Srb36gZZN{[Xl?		NEHP[\|EyNjViaILz		MVjJcohq[mm2aX;uJI9nKEGtdEGgbY4hcHWvYX6gUG5ESVBiY3XscJMh[XO\|ZYPz[YQh[XNicHjvd5Bpd3K7bHH0bY9vKG:oIGDSRXM1OCCjdDDUbJIzPDZiYX\0[ZIhOS53IHjyd{whUUN3MDC9JFAvOTV5IN88UU4>	NH7VN4M9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{MkmzOFU4PSd-MkK5N\|Q2PzV:L3G+
PC3	M3nXSmZ2dmO2aX;uJIF{e2G7	MVG1NEBu\y:tZx?=	NGTFUZY6KGi{cx?=		Mk\kVIxie22jIHPvcoNmdnS{YYTpc44hcW5iboWvcpUhdW:3c3WgfIVvd2e{YX\0[YQhf2m2aDDoeY1idiCSQ{OgZ4VtdHNiYYSgOVAhdWdxa3esJJBwKGG2IEmgbJJ{KGK7IFzDM21UN02VIHHuZYx6e2m\|LDDDdEA:KDBwNTFOwG0v	Mn63QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O\|UoRjJ{OUO0OVc2RC:jPh?=
BT474M1	M4O1S2N6fG:2b4jpZ4l1gSCjc4PhfS=>		NIPoSpQ6PiCqcoO=		NHLrfmxEgXSxdH;4bYNqfHliYXfhbY5{fCCqdX3hckBDXDR5NF2xJINmdGy\|IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEm2JIhzeyCkeTDD[YxtXGm2cnWtS4xwKGG\|c3H5MEBKSzVyIE2gNUDPxE1w	NVfGWm11RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N\|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3	NWG0WGtUS3m2b4TvfIlkcXS7IHHzd4F6		M{S0eVk3KGi{cx?=		M3HsNGN6fG:2b4jpZ4l1gSCjZ3HpcpN1KGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjDj[YxtKH[rYXLpcIl1gSCjZoTldkA6PiCqcoOgZpkhS2WubGTpeJJmNUeubzDhd5NigSxiSVO1NEA:KDFizszNMi=>	MnXiQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O\|UoRjJ{OUO0OVc2RC:jPh?=
MCF7	M37aeWN6fG:2b4jpZ4l1gSCjc4PhfS=>		NEPlZ3g6PiCqcoO=		NVzUV3U6S3m2b4TvfIlkcXS7IHHnZYlve3RiaIXtZY4hVUOINzDj[YxteyCxdnXy[ZhxemW\|c3nu[{BJ\XJ{IHHzd4V{e2WmIHHzJIRm[3KnYYPlJIlvKGOnbHygeoli[mmuaYT5JIFnfGW{IEm2JIhzeyCkeTDD[YxtXGm2cnWtS4xwKGG\|c3H5MEBKSzVyIE2gNUDPxE1w	NU\hbHlrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N\|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3	NWDlOJBXTnWwY4Tpc44h[XO\|YYm=	MUi1NEBu\y:tZx?=	NHnQWoMyKGi{		M1rhbXBt[XOvYTDjc45k\W62cnH0bY9vKGmwIH71M452KG2xdYPlJJhmdm:pcnHmeIVlKHerdHigbJVu[W5iUFOzJINmdGy\|IHH0JFUxKG2pL3vnMEBxdyCjdDCxJIhzKGK7IFzDM21UN02VIHHuZYx6e2m\|LDDDdEA:KDdwNDFOwG0v	MYe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl\|NEW3OUc,OjJ7M{S1O\|U9N2F-
PC3	NX30RlNsTnWwY4Tpc44h[XO\|YYm=	MWCxNFAhdWdxa3e=	NXLBR41kQCCqcoO=		MU\Jcohq[mm2aX;uJI9nKEGtdDDpckBvfS:wdTDtc5V{\SC6ZX7v[5Ji\nSnZDD3bZRpKGi3bXHuJHBEOyClZXzsd{Bie3Onc4Pl[EBieyCmZXPy[YF{\SCrbjD0eY1weiCyLWO2VnAhdGW4ZXygZZQhOTByIH3nM4toNCCybzDheEA5KGi{czDifUBGVEmVQTDy[YxifGm4ZTD0c{B1d3SjbDDTOnJR	Mk[xQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjJ7M{S1O\|UoRjJ{OUO0OVc2RC:jPh?=
MCF7	NEHZZ3RHfW6ldHnvckBie3OjeR?=				NGKy[nZKdmirYnn0bY9vKG:oIFHreFEudWWmaXH0[YQhWFKDU{SwJJBpd3OyaH;yfYxifGmxbjDpckBpfW2jbjDNR2Y4KGOnbHzzJI93\XKneIDy[ZN{cW6pIFjldlI>	NX[wfnRsRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N\|Q2PzVpPkKyPVM1PTd3PD;hQi=>
BT474M1	NIHJOFNHfW6ldHnvckBie3OjeR?=				MmmxTY5pcWKrdHnvckBw\iCDa4SxMY1m\GmjdHXkJHBTSVN2MDDwbI9{eGixconsZZRqd25iaX6gbJVu[W5iQmS0O\|ROOSClZXzsdy=>	NXnRTWp5RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkK5N\|Q2PzVpPkKyPVM1PTd3PD;hQi=>
PC3	MoL6SpVv[3Srb36gZZN{[Xl?				MYTJcohq[mm2aX;uJI9nKEGtdEGtcYVlcWG2ZXSgVHJCWzRyIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCSQ{OgZ4VtdHN?	MVi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl\|NEW3OUc,OjJ7M{S1O\|U9N2F-
LNCAP	M3L6XmZ2dmO2aX;uJIF{e2G7				MYjJcohq[mm2aX;uJI9nKEGtdEGtcYVlcWG2ZXSgVHJCWzRyIIDoc5NxcG:{eXzheIlwdiCrbjDoeY1idiCOTlPBVEBk\Wyucx?=	MWi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zOjl\|NEW3OUc,OjJ7M{S1O\|U9N2F-
A673	NULqfIRGeUiWUzDhd5NigQ>?				NU\3eGR2eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFG2O\|Mh[2WubIO=	M3XXSlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
DAOY	MXzxTHRUKGG\|c3H5				NYjF[Ww{eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC\|Y4Ll[Y4h\m:{IFTBU3kh[2WubIO=	MVK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
Saos-2	NIP5WohyUFSVIHHzd4F6				M17IUZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVYX;zMVIh[2WubIO=	MoDoQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
BT-37	MkjXdWhVWyCjc4PhfS=>				MX\xTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhSlRvM{egZ4VtdHN?	M2i2fVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ7NEO1NVM6Lz5{OUSzOVE{QTxxYU6=
RD	NYLBTG1QeUiWUzDhd5NigQ>?				MXHxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW\|IH\vdkBlenWpIILldJVzeG:\|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhWkRiY3XscJM>	MUK8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR\|NUGzPUc,Ojl2M{WxN\|k9N2F-
SK-N-SH	M1zrdJFJXFNiYYPzZZk>				M2HEdJFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCVSz3OMXNJKGOnbHzz	NXzqTldMRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkm0N\|UyOzlpPkK5OFM2OTN7PD;hQi=>
BT-12	MXHxTHRUKGG\|c3H5				Ml;QdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[\|ohWHKrbXHyfUB{[3KnZX6g[o9zKEKWLUGyJINmdGy\|	MmjMQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN\|koRjJ7NEO1NVM6RC:jPh?=
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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 ; cleaved-caspase3 ; Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1 ; p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 ; PUMA

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 (from reference)

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

References

+ Expand

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	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O

Download Ipatasertib (GDC-0068) SDF

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:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

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

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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