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Cat. No. M1862
GDC-0068 Structure

Ipatasertib, RG7440

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mg USD 170 In stock
50mg USD 480 In stock
100mg USD 650 In stock
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Quality Control
Biological Activity

GDC-0068 (RG7440) is a novel, ATP-competitive and orally bioavailable Akt inhibitor with IC50 values of 5 nM, 18 nM and 8 nM for Akt1, Akt2 and Akt3, respectively. Ipatasertib (GDC-0068) demonstrates potent inhibition of all three Akt isoforms in biochemical assays, but poor inhibition of other AGC family kinases. Moreover, GDC-0068 selectively inhibits cell cycle progression and viability of cancer cell lines driven by PI3K/Akt signaling pathway, including those with defects in the tumor suppressor PTEN, oncogenic mutations in PIK3CA, and amplification of HER2. GDC-0068 (Ipatasertib) blocks the phosphorylation of multiple downstream targets of Akt in human cancer cell lines. GDC-0068 (RG7440) shows good oral exposure resulting in dose-dependent pharmacodynamic effects on downstream biomarkers and a robust anti-tumor response in xenograft models in which the PI3K-Akt-mTOR pathway is activated.

Customer Product Validations & Biological Datas
Source Clin Cancer Res (2013). Figure 1.GDC-0068
Method Western blot
Cell Lines IGROV-1 cell
Concentrations 200 nmol/L
Incubation Time 4 h
Results GDC-0068 showed more than 600 and more than 100-fold selectivity for Akt1 in IC50 against the closely related kinases PKA and p70S6K, respectively
Cell Experiment
Cell lines MCF10A cells with or without PTEN knockout (KO)
Preparation method Cell viability assays The 384-well plates were seeded with 2,000 cells per well in a volume of 54 μL per well followed by incubation at 37°C under 5% CO2 overnight (∼16 hours). Compounds were diluted in dimethyl sulfoxide (DMSO) to generate the desired stock concentrations then added in a volume of 6 μL per well. All treatments were tested in quadruplicates. After 4 days incubation, relative numbers of viable cells were estimated using CellTiter-Glo (Promega) and total luminescence was measured on a Wallac Multilabel Reader (PerkinElmer). The concentration of drug resulting in IC50 was calculated from a 4-parameter curve analysis (XLfit, IDBS software) and was determined from a minimum of 3 experiments. For cell lines that failed to achieve an IC50, the highest concentration tested (10 μmol/L) is listed.
Concentrations 0~10µM
Incubation time 4 days
Animal Experiment
Animal models MCF7-neo/HER2 tumor xenograft model
Formulation 0.5% methylcellulose/0.2% Tween-80 (MCT)
Dosages 0,12.5, 25, 50, 75, 100mg/kg
Administration oral gavage
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 458
Formula C24H32ClN5O2
CAS Number 1001264-89-6
Purity 99.25%
Solubility DMSO ≥90 mg/mL
Ethanol ≥90 mg/mL
Storage at -20°C

Discovery and Preclinical Pharmacology of a Selective ATP-competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors.
Blake et al. J Med Chem. 2012 Aug 30. PMID: 22934575.

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Abmole Inhibitor Catalog 2017

Keywords: GDC-0068, Ipatasertib, RG7440 supplier, Akt, inhibitors

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