Home PI3K/Akt/mTOR Akt inhibitor Ipatasertib (GDC-0068) For research use only.

Ipatasertib (GDC-0068)

Synonyms: RG7440

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.

Ipatasertib (GDC-0068) Chemical Structure

Ipatasertib (GDC-0068) Chemical Structure

CAS No. 1001264-89-6

Purity & Quality Control

Ipatasertib (GDC-0068) Related Products

Signaling Pathway

Akt Signaling Pathways

Akt Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCC70  Function Assay 1 μM 24 h increases the abundance of HER3 and induces the phosphorylation (activation) of both EGFR and HER3 24667376
MDA-MB-468  Function Assay 1 μM 24 h increases the abundance of HER3 24667376
HCC70  Growth Inhibition Assay 1 μM 5 d enhances the antiproliferative response 24667376
MDA-MB-468  Growth Inhibition Assay 1 μM 5 d enhances the antiproliferative response 24667376
PC-3 Function Assay 0.0038-2.5 μM 1 h DMSO induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473 23287563
BT474M1 Function Assay 0.0038-2.5 μM 1 h DMSO induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473 23287563
IGROV-1 Function Assay 0.0038-2.5 μM 1 h DMSO induces a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser473 23287563
PC-3 Growth Inhibition Assay 1/5/10 μM 24/48/72 h DMSO dose-dependently increases the G0–G1 phase population  23287563
MCF7-neo/HER2 Growth Inhibition Assay 1/5/10 μM 24/48/72 h DMSO dose-dependently increases the G0–G1 phase population  23287563
BT474M1 Growth Inhibition Assay 1/5/10 μM 24/48/72 h DMSO dose-dependently increases the G0–G1 phase population  23287563
PC-3 Apoptosis Assay 1/5/10 μM 15/48/72 h DMSO causes a dose- and time-dependent increase in apoptotic and necrotic populations 23287563
MCF7-neo/HER2 Apoptosis Assay 1/5/10 μM 15/48/72 h DMSO causes a dose- and time-dependent increase in apoptotic and necrotic populations 23287563
BT474M1 Apoptosis Assay 1/5/10 μM 15/48/72 h DMSO causes a dose- and time-dependent increase in apoptotic and necrotic populations 23287563
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells assessed as reduction of resazurin to resorufin after 72 hrs, IC50 = 0.095 μM. 22934575
LNCAP Function assay 1.5 hrs Inhibition of Akt1 in human LNCAP cells assessed as phosphorylation of PRAS40 at Thr246 after 1.5 hrs, IC50 = 0.157 μM. 22934575
PC3 Function assay 50 mg/kg 9 hrs Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po at 9 hrs by LC/MS/MS analysis, Cp = 0.5 μM. 22934575
BT474M1 Cytotoxicity assay 96 hrs Cytotoxicity against human BT474M1 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay, IC50 = 1 μM. 22934575
PC3 Cytotoxicity assay 96 hrs Cytotoxicity against human PC3 cells assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay, IC50 = 1 μM. 22934575
MCF7 Cytotoxicity assay 96 hrs Cytotoxicity against human MCF7 cells overexpressing Her2 assessed as decrease in cell viability after 96 hrs by CellTitre-Glo assay, IC50 = 1 μM. 22934575
PC3 Function assay 50 mg/kg 1 hr Plasma concentration in nu/nu mouse xenografted with human PC3 cells at 50 mg/kg, po at 1 hr by LC/MS/MS analysis, Cp = 7.4 μM. 22934575
PC3 Function assay 100 mg/kg 8 hrs Inhibition of Akt in nu/nu mouse xenografted with human PC3 cells assessed as decrease in tumor p-S6RP level at 100 mg/kg, po at 8 hrs by ELISA relative to total S6RP 22934575
MCF7 Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human MCF7 cells overexpressing Her2 22934575
BT474M1 Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human BT474M1 cells 22934575
PC3 Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human PC3 cells 22934575
LNCAP Function assay Inhibition of Akt1-mediated PRAS40 phosphorylation in human LNCAP cells 22934575
A673 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells 29435139
DAOY qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
BT-37 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells 29435139
RD qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells 29435139
BT-12 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells 29435139
NB1643 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for LAN-5 cells 29435139
SK-N-SH qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells 29435139
MG 63 (6-TG R) qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for MG 63 (6-TG R) cells 29435139
Rh30 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells 29435139
Rh41 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells 29435139
SJ-GBM2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
NB-EBc1 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells 29435139
LAN-5 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells 29435139
Rh18 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells 29435139
SK-N-MC qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells 29435139
TC32 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells 29435139
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells 29435139
Click to View More Cell Line Experimental Data

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot PUMA p-AKT / AKT / p-FoxO3a / FoxO3a / p-p65 / p65 Noxa / Bid / Bad / Bim / Bcl-2 / Bcl-xl / Mcl-1 cleaved-caspase3 p-PRAS40(T246) / PRAS40 / p-ERK / ERK / pFOXO1 / pFOXO3a / pGSK3b(S9) / pAS160(S318) / pBAD(S136) / pS6 / p4E-BP1 30185800
In Vivo
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 Animal Models Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
Dosages ~100 mg/kg/day
Administration Orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01090960 Completed
Solid Cancers
Genentech Inc.
 March 2010 Phase 1

Chemical Information & Solubility

Molecular Weight 458 Formula

C24H32ClN5O2
CAS No. 1001264-89-6 SDF Download Ipatasertib (GDC-0068) SDF
Smiles CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (198.68 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 91 mg/mL

Water : Insoluble


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In vivo
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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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