GDC-0349

Catalog No.S8040 Synonyms: RG-7603

For research use only.

GDC-0349 (RG-7603) 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.

GDC-0349 Chemical Structure

CAS No. 1207360-89-1

Selleck's GDC-0349 has been cited by 3 Publications

1 Customer Review

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Biological Activity

Description GDC-0349 (RG-7603) 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]

Assay
Methods Test Index PMID
Western blot p-AKT / AKT1 / p-S6K / S6K1 / LC3B-II / ATG-7 / Beclin-1 / p62 27291151
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 (from reference)

Animal Research: [1]
  • Animal Models: MCF7-neo/Her2 tumor xenograft
  • Dosages: 10, 20, 30, 40,50, 60, 70, 80 mg/kg
  • Administration: orally

Solubility (25°C)

In vitro

DMSO 91 mg/mL
(201.08 mM)
Ethanol 6 mg/mL
(13.25 mM)
Water Insoluble

Chemical Information

Molecular Weight 452.55
Formula

C24H32N6O3

CAS No. 1207360-89-1
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4COC4)C(=N2)N5CCOCC5C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT01356173 Completed Drug: GDC-0349 Non-Hodgkin''s Lymphoma Solid Tumor Genentech Inc. June 2011 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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

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