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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3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
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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.
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]


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 <1 mg/mL
In vivo

* 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 Information

Molecular Weight 452.55


CAS No. 1207360-89-1
Storage powder
in solvent
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

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mTOR Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID