GDC-0068, Akt Inhibitor


Catalog No. size PriceQuantity
M60066-5S 5mg solid $159
M60066-50S 50 mg solid $1,060

Description

Product Information
Molecular Weight: 458.00
Formula: C24H32ClN5O2
Purity: ≥98%
CAS#: 1001264-89-6
Solubility: DMSO up to 100 mM
Chemical Name: (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one
Storage: Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year.

 

Biological Activity:

GDC-0068 is a highly potent, selective, and orally available pan-Akt inhibitor, targeting Akt1, Akt2 and Akt3 with IC50 of 5 nM, 18 nM and 8 nM, respectively. It has >100-fold selectivity over a broad panel of 230 kinases, except PRKG1α and PRKG1β with IC50 of 98 nM and 69 nM. GDC-0068 can effectively block Akt signaling and induce cell cycle arrest in human cancer cell lines in vitro, and exhibit significant efficacy in PTEN- and PI3K mutant xenograft models, including PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. A Phase I study of GDC-0068 in patients with refractory solid tumors is ongoing.

How to Use: 

  • In vitro:  GDC-0068 was used at 5-10 µM final concentration in vitro and in cellular assays.
  • In vivo: GDC-0068 was orally dosed to mice at 50-100 mg/kg once per day, or in combination with MEK inhibitors or chemotherapy agents to significantly reduce the tumor volume. Formulation: 0.5% methylcellulose/0.2% Tween-80.

Reference: 

  • 1. Blake JF, et al. Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors. (2012) J Med Chem. 55(18):8110-27.
  • 2. Heidi M, et al. Abstract 966: Predictive biomarkers of the AKT inhibitor, GDC-0068, in single agent and combination studies. (2012) Cancer Research. Volume 72, Issue 8, Supplement 1
  • 3. Kui Lin. Abstract DDT02-01: GDC-0068: A novel, selective, ATP-competitive inhibitor of Akt. (2011) Cancer Research. Volume 71, Issue 8, Supplement 1
  • 4. http://www.arraybiopharma.com/_documents/Publication/PubAttachment437.pdf

 

Products are for research use only. Not for human use. 

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