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GDC-0068 (RG7440)

Catalog No.
Pan-AKT inhibitor,highly selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
In stock
Evaluation Sample
In stock
In stock
In stock
In stock
In stock

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Email: [email protected]

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GDC-0068 (RG7440) is a highly selective small molecule inhibitor of Akt with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3. The PI3K-AKT pathway regulates cell growth, survival and tumorigenesis. GDC-0068 binds to and blocks the activation of AKT, which result in cell cycle arrest, inhibition of tumor cell proliferation and induction of tumor cell death. PI3K-AKT is pathway frequently activated in tumors, thus tumors with PTEN or PI3K mutations, which lead to activation of AKT are with high sensitivity to GDC-0068. GDC-0068 is now used for the treatment of human cancers.


1. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. JF Blake, R Xu, JR Bencsik, D Xiao… - Journal of medicinal  2012

2. Lin J, Sampath D, Nannini MA, et al: Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Canc Res 2013, 19:1760–1772.

Product Citation

Chemical Properties

Physical AppearanceA solid
StorageDesiccate at -20°C
Cas No.1001264-89-6
Solubility≥22.9 mg/mL in DMSO; insoluble in H2O; ≥28.35 mg/mL in EtOH
Chemical Name(2S)-2-(4-chlorophenyl)-1-[4-[(5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl]piperazin-1-yl]-3-(propan-2-ylamino)propan-1-one
SDFDownload SDF
Canonical SMILESCC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O
Shipping ConditionEvaluation sample solution: ship with blue ice. All other available sizes: ship with RT, or blue ice upon request.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. Stock solution can be stored below -20°C for several months.


Cell experiment [1]:

Cell lines

PC-3, BT474M1 and IGROV-1 cell lines

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

1 h; 25 μmol/L


The biologic activity of GDC-0068 was evaluated in cell-based assays in vitro . Similar to other ATP-competitive Akt inhibitors, GDC-0068 induced a dose-dependent increase in Akt phosphorylation at both Thr308 (T308) and Ser 473 (S473) residues in all cell lines tested, including lines in which the PI3K/Akt pathway is activated, such as PC-3 (PTEN homozygous deletion mutant, prostate), BT474M1 (PIK3CAK111N mutant and HER2-amplified, breast), IGROV-1 (PTENT319fsX1/Y155C and PIK3CA1069 W, ovarian).

Animal experiment [1]:

Animal models

Nude mice

Dosage form

100 mg//kg; Oral taken


The in vitro sensitivity profile of GDC-0068 was recapitulated in vivo in xenograft models representing a spectrum of cancer types including prostate, breast, ovarian, colorectal, non–small cell lung, glioblastoma, and melanoma. GDC-0068 was typically efficacious in xenograft models in which Akt was activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression was achieved at or below 100 mg/kg daily oral dose, which was the maximum dose tested in immunocompromised mice that was well tolerated.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.


[1] Lin J, Sampath D, Nannini M A, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models[J]. Clinical Cancer Research, 2013, 19(7): 1760-1772.

Biological Activity

Description Ipatasertib (GDC-0068) is a highly selective inhibitor of Akt for Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA.
Targets Akt1 Akt2 Akt3      
IC50 5 nM 18 nM 8 nM      

Quality Control

Chemical structure

GDC-0068 (RG7440)

Related Biological Data

GDC-0068 (RG7440)