GDC-0349

Catalog No.S8040 Synonyms: RG-7603

GDC-0349 Chemical Structure

Molecular Weight(MW): 452.55

GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.

Size Price Stock Quantity  
In DMSO USD 380 In stock
USD 210 In stock
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  • The established (SQ20B/UMSCC47/SCC90 cells) or primary (“P1/P2/P3”) human NSCC cells as well as normal oral epithelial cells (“Epithelial cells”) were treated with indicated concentration of GDC-0349, rapamycin (“Rap”) or RAD001 for applied time, cell proliferation was tested by CCK-8 assay. Expression of listed proteins in primary human NSCC cells was tested by Western blot analysis (D, right panel). “UNTR” indicates untreated control cells. * p < 0.05 vs. “UNTR” cells. # p < 0.05 vs. GDC-0349-only cells.

    Biochem Biophys Res Commun, 2016, 477(2):174-80.. GDC-0349 purchased from Selleck.

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Biological Activity

Description GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM, 790-fold inhibitory effect against PI3Kα and other 266 kinases. Phase 1.
Targets
mTOR [1] PI3Kα [1]
3.8 nM(Ki) ~3 μM(Ki)
In vitro

GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. GDC-0349 inhibits downstream markers of mTOR, including phospho-4EBP1 and phospho-Akt(S473) in an in vivo PK/PD study in mouse, consistent with an inhibition of both mTORC1 and mTORC2 complexes. [1]

In vivo GDC-0349 demonstrates pathway modulation and dose-dependent efficacy in mouse xenograft cancer models. When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 inhibits tumor growth in a dose-dependent manner. It is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-O (VHL mutant). [1]

Protocol

Animal Research: [1]
+ Expand
  • Animal Models: MCF7-neo/Her2 tumor xenograft
  • Formulation: 0.5% methylcellulose/0.2% Tween 80
  • Dosages: 10, 20, 30, 40,50, 60, 70, 80 mg/kg
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 91 mg/mL (201.08 mM)
Ethanol 6 mg/mL (13.25 mM)
Water 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 452.55
Formula

C24H32N6O3

CAS No. 1207360-89-1
Storage powder
Synonyms RG-7603

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01356173 Completed Non-Hodgkins Lymphoma, Solid Tumor Genentech, Inc. June 2011 Phase 1

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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID