GDC-0068

Catalog No.S2808

GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. Phase 2.

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GDC-0068 Chemical Structure

GDC-0068 Chemical Structure
Molecular Weight: 458

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

GDC-0068 is available in the following compound libraries:

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Product Information

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  • Research Area
  • Combination Therapy
    Combination Therapy

Product Description

Biological Activity

Description GDC-0068 is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM, 620-fold selectivity over PKA. Phase 2.
Targets Akt1 Akt3 Akt2
IC50 5 nM [1] 8 nM [1] 18 nM [1]
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]
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]
Features

Protocol(Only for Reference)

Animal Study: [1]

Animal Models Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
Formulation Formulated in 0.5% methylcellulose/0.2% Tween-80
Dosages ~100 mg/kg/day
Administration Orally
1

References

[1] Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.

[2] James F. Blake. 2011.

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Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT01362374 Recruiting Solid Cancers Genentech 2011-07 Phase 1
NCT01485861 Recruiting Prostate Cancer Genentech 2011-12 Phase 2
NCT01562275 Recruiting Neoplasms Genentech 2012-04 Phase 1
NCT01896531 Recruiting Gastric Cancer Genentech 2013-08 Phase 2
NCT02063581 Completed Healthy Volunteer Genentech 2014-02 Phase 1

Chemical Information

Download GDC-0068 SDF
Molecular Weight (MW) 458
Formula

C24H32ClN5O2

CAS No. 1001264-89-6
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Synonyms RG7440
Solubility (25°C) * In vitro DMSO 92 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol 92 mg/mL (200 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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

Research Area

Tech Support & FAQs

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.

Tel: +1-832-582-8158 Ext:3

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