Loading... Please wait...

Categories

Our Newsletter


GDC-0068 | Pan-Akt inhibitor

  • GDC-0068.jpg
  • GDC-0068, 400x400px, png
Price:
$159.00
Catalog #:
C4006-2s
Quantity:


Product Description

GDC-0068 is a potent, highly selective, orally available, ATP-competitive pan-AKT inhibitor, targeting Akt1, Akt2 and Akt3 with IC50 of 5 nM, 18 nM and 8 nM, respectively. It demonstrates high selectivity
over more than 200 screened kinases, with >100 fold selectivity for Akt over PKA [1-4].

Akt functions as a central role of the PI3K-Akt-mTOR pathway. It is one of the most frequently activated protein serine/threonine kinases in human malignancies. Inhibiting Akt activity has become an attractive approach for cancer treatment. GDC-0068 blocks the phosphorylation of multiple downstream targets of Akt in human cancer cell lines in a dose-dependent manner. It inhibits cell cycle progression and viability of cancer cell lines, most robustly in cells with activated PI3K-Akt-mTOR pathway driven by PIK3CA , PTEN loss and HER2 amplification. GDC-0068 treatment results in pronounced PD effects in tumor xenograft models including dose dependent suppression of p-PRAS40, P-S6 and P-eIF4G, as well as induction of FOXO nuclear localization. GDC-0086 has exhibited antitumor efficacy in multiple xenograft tumor models. In addition, consistent with the role of Akt in a survival pathway, GDC-0068 also demonstrates enhanced antitumor efficacy when combined with other therapeutic agents. GDC-0068 is currently in Phase 1a and Phase 1b clinical development in cancer patients [1-4].


Technical information:

Chemical Formula:   C24H32ClN5O2
CAS #:   0
Molecular Weight:   458
Purity:   > 98%
Appearance:   White
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
Solubility:   Up to 100 mM in DMSO
Synonyms:   GDC-0068, GDC0068

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.


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. J Med Chem. 2012. 55(18):8110-27. Pubmed ID: 22934575
2. Lin K. GDC-0068: A novel, selective, ATP-competitive inhibitor of Akt. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.
3. Blake JF. Discovery of GDC-0068: A Selective ATP-competitive Akt Inhibitor for the Treatment of Human Tumors. CHI Next Generation Kinase Inhibitors. June 6-8, 2011. http://www.arraybiopharma.com/_documents/Publication/PubAttachment478.pdf
4. Abernero J, et al. Targeting the PI3K-Akt-mTOR pathway with GDC-0068, a novel selective ATP competitive Akt inhibitor. http://www.arraybiopharma.com/_documents/Publication/PubAttachment437.pdf

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.

Write your own product review

Product Reviews

This product hasn't received any reviews yet. Be the first to review this product!

Add to Wish List

Click the button below to add the GDC-0068 | Pan-Akt inhibitor to your wish list.

You Recently Viewed...