GDC-0084

Catalog No.S8163

GDC-0084 Chemical Structure

Molecular Weight(MW): 382.42

GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.

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Biological Activity

Description GDC-0084 is a brain penetrant inhibitor of PI3K and mTOR.
Targets
PI3Kα [1]
(Cell-free assay)
PI3Kδ [1]
(Cell-free assay)
PI3Kγ [1]
(Cell-free assay)
PI3Kβ [1]
(Cell-free assay)
mTOR [1]
(Cell-free assay)
2 nM(Ki) 3 nM(Ki) 10 nM(Ki) 46 nM(Ki) 70 nM(Ki)
In vitro

GDC-0084 has excellent human metabolic stability in microsomal and hepatocyte incubations and demonstrated inhibition of pAKT, a key signal within the PI3K pathway, in normal brain tissue[1]. GDC-0084 is shown to inhibit the proliferation of several glioma cells in vitro with IC50 ranging from 0.3 to 1.1 μM. GDC-0084 binding to plasma proteins is low, with a free fraction (%) of 29.5±2.7 (n=3) in CD-1 mouse plasma, when tested at 5 μM. Binding to brain tissues from CD-1 mice is higher, with a free fraction of 6.7% (±1; n=3)[2].

In vivo GDC-0084 markedly inhibits the PI3K pathway in mouse brain, causing up to 90% suppression of the pAkt signal. GDC-0084 achieves significant tumor growth inhibition of 70% and 40% against the U87 and GS2 orthotopic models, respectively. GDC-0084 distribution throughout the brain and intracranial tumors leads to potent inhibition of the PI3K pathway. It is being evaluated in patients, and exposures reached at tolerated doses are consistent with those associated with efficacious doses in mouse models[2].

Protocol

Cell Research:[2]
+ Expand
  • Cell lines: Madin-Darby canine kidney (MDCK) cells (MDR1-MDCKI cells)
  • Concentrations: 5 μM
  • Incubation Time: 2 h
  • Method: For transport studies, cells are seeded on 24-well Millicell plates 4 days prior to use(polyethylene terephtalate membrane, 1 μm pore size) at a seeding density of 1.3×105 cells/ml). GDC-0084 is tested at 5 μM in the apical-tobasolateral (A-B) and basolateral-to-apical (B-A) directions. The compound is dissolved in transport buffer consisting of Hanks' balanced salt solution with 10 mM HEPES. Lucifer Yellow is used as the paracellular and monolayer integrity marker. GDC-0084 concentrations in the donor and receiving compartments are determined by liquid chromatography-tandem mass spectrometry (LC-MS/MS) analysis. The apparent permeability (Papp), in the apical to A-B and B-A directions, is calculated after 2-hour incubation.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: Male Sprague−Dawley rats or female CD-1 mice
  • Formulation: 60% PEG400/10% ethanol(i.v.) or 0.5% methylcellulose with 0.2% Tween 80(p.o.)
  • Dosages: 1 mg/kg(i.v.);5 or 25 mg/kg(p.o.)
  • Administration: i.v. or p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 8 mg/mL (20.91 mM)
Water Insoluble
Ethanol 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 Information

Molecular Weight 382.42
Formula

C18H22N8O2

CAS No. 1382979-44-3
Storage powder
Synonyms N/A

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Tech Support

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.

Handling Instructions

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

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PI3K Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID