Ipatasertib (GDC-0068)

Catalog No.S2808 Synonyms: RG7440

Ipatasertib (GDC-0068) Chemical Structure

Molecular Weight(MW): 458

Ipatasertib (GDC-0068) 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.

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In DMSO USD 378 In stock
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Cited by 20 Publications

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Biological Activity

Description Ipatasertib (GDC-0068) 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.
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  NFe4dWtHfW6ldHnvckBCe3OjeR?= M3nnfFEh|ryP M3HIOVI1KGh? M3HISYlv[3KnYYPld{B1cGViYXL1coRidmOnIH;mJGhGWjNiYX7kJIlv\HWlZYOgeIhmKHCqb4PwbI9zgWyjdHnvckAp[WO2aY\heIlwdilib3[gZo91cCCHR1\SJIFv\CCKRWKz NEHWO5AzPDZ4N{O3Oi=>
MDA-MB-468  M4f6eWZ2dmO2aX;uJGF{e2G7 M3W0R|Eh|ryP NVewSphnOjRiaB?= MoHEbY5kemWjc3XzJJRp\SCjYoXu[IFv[2Vib3[gTGVTOw>? MlXpNlQ3Pjd|N{[=
HCC70  MnfaS5Jwf3SqIFnubIljcXSrb36gRZN{[Xl? NWPyfIgyOSEQvF2= MoXxOUBl Ml34[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKHKnc4DvcpNm M{fme|I1PjZ5M{e2
MDA-MB-468  NGjOcWVIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= MY[xJO69VQ>? NVX5O3RyPSCm MmDZ[Y5p[W6lZYOgeIhmKGGwdHnwdo9tcW[ncnH0bZZmKHKnc4DvcpNm MXyyOFY3PzN5Nh?=
PC-3 M2HPVGZ2dmO2aX;uJGF{e2G7 MYmwMlAxOzhvMj61JO69VQ>? NGjp[GIyKGh? M4Oz[WROW09? NIX6S45qdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> NHPRfGczOzJ6N{W2Ny=>
BT474M1 MX7GeY5kfGmxbjDBd5NigQ>? M1LKb|AvODB|OD2yMlUh|ryP M2jrU|EhcA>? NEfhRo9FVVOR NGixUXNqdmS3Y3XzJIEh\G:|ZT3k[ZBmdmSnboSgbY5kemWjc3WgbY4hSWu2IIDoc5NxcG:{eXzheIlwdiCjdDDic5RpKFSqckOwPOKhMFR|MEipJIFv\CCVZYK0O|M> NVXycoI1OjN{OEe1OlM>
IGROV-1 NXW0TGpITnWwY4Tpc44hSXO|YYm= M1zBZVAvODB|OD2yMlUh|ryP NIPpdWIyKGh? NV\IfXdLTE2VTx?= Ml6ybY5lfWOnczDhJIRwe2VvZHXw[Y5l\W62IHnuZ5Jm[XOnIHnuJGFsfCCyaH;zdIhwenmuYYTpc44h[XRiYn;0bEBVcHJ|MElCpEhVOzB6KTDhcoQhW2W{NEez MoTSNlMzQDd3NkO=
PC-3 NUO0SphkT3Kxd4ToJGlvcGmkaYTpc44hSXO|YYm= NEf5fVIyNzVxMUCg{txO NXXKWlZwOjRxNEivO|IhcA>? NEfJeZJFVVOR NX:wO4Mz\G:|ZT3k[ZBmdmSnboTsfUBqdmO{ZXHz[ZMhfGinIFew5qCUTzIEoIDoZZNmKHCxcIXsZZRqd28EoB?= MXuyN|I5PzV4Mx?=
MCF7-neo/HER2 NFX3NVFIem:5dHigTY5pcWKrdHnvckBCe3OjeR?= M3\tZ|EwPS9zMDFOwG0> NI\LVnczPC92OD:3NkBp MVfEUXNQ MUXkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh NUnuWlVCOjN{OEe1OlM>
BT474M1 M{Xzbmdzd3e2aDDJcohq[mm2aX;uJGF{e2G7 MWGxM|UwOTBizszN MWWyOE81QC95MjDo M1zSOGROW09? MXjkc5NmNWSncHXu[IVvfGy7IHnuZ5Jm[XOnczD0bIUhTzEkgKPHNeKheGijc3WgdI9xfWyjdHnvcuKh NEe0N5MzOzJ6N{W2Ny=>
PC-3 M1LwV2Fxd3C2b4Ppd{BCe3OjeR?= MUKxM|UwOTBizszN MlezNVUwPDhxN{KgbC=> MoDkSG1UVw>? MXfjZZV{\XNiYTDkc5NmNSCjbnSgeIlu\S2mZYDlcoRmdnRiaX7jdoVie2ViaX6gZZBweHSxdHnjJIFv\CCwZXPyc5Rq[yCyb4D1cIF1cW:wcx?= NUPMfIxKOjN{OEe1OlM>
MCF7-neo/HER2 M4q1d2Fxd3C2b4Ppd{BCe3OjeR?= NIX0PI0yNzVxMUCg{txO MnfrNVUwPDhxN{KgbC=> M3XOfGROW09? M{\BSoNifXOnczDhJIRwe2VvIHHu[EB1cW2nLXTldIVv\GWwdDDpcoNz\WG|ZTDpckBieG:ydH;0bYMh[W6mIH7lZ5JwfGmlIIDvdJVt[XSrb37z Mnn3NlMzQDd3NkO=
BT474M1 NHKwcHBCeG:ydH;zbZMhSXO|YYm= NHH3Nm0yNzVxMUCg{txO MoPiNVUwPDhxN{KgbC=> NXXZUlRtTE2VTx?= NVr0WWVQ[2G3c3XzJIEh\G:|ZT2gZY5lKHSrbXWt[IVx\W6mZX70JIlv[3KnYYPlJIlvKGGyb4D0c5Rq[yCjbnSgcoVkem:2aXOgdI9xfWyjdHnvcpM> MnL3NlMzQDd3NkO=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot

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. 


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
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]


Animal Research:[1]
+ Expand
  • Animal Models: Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
  • Formulation: Formulated in 0.5% methylcellulose/0.2% Tween-80
  • Dosages: ~100 mg/kg/day
  • Administration: Orally
    (Only for Reference)

Solubility (25°C)

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

* 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


CAS No. 1001264-89-6
Storage powder
in solvent
Synonyms RG7440

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID