Home PI3K/Akt/mTOR mTOR inhibitor GDC-0349 For research use only.

GDC-0349

Synonyms: RG-7603

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

GDC-0349 Chemical Structure

CAS No. 1207360-89-1

Purity & Quality Control

Batch: S804001 DMSO]91 mg/mL]false]Ethanol]6 mg/mL]false]Water]Insoluble]false Purity: 99.01%
99.01

GDC-0349 Related Products

Signaling Pathway

mTOR Signaling Pathways

mTOR Signaling Pathway

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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-AKT / AKT1 / p-S6K / S6K1 / LC3B-II / ATG-7 / Beclin-1 / p62 27291151
In Vivo
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 Animal Models MCF7-neo/Her2 tumor xenograft
Dosages 10, 20, 30, 40,50, 60, 70, 80 mg/kg
Administration orally
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01356173 Completed
Non-Hodgkin''s Lymphoma Solid Tumor
Genentech Inc.
 June 2011 Phase 1

Chemical Information & Solubility

Molecular Weight 452.55 Formula

C24H32N6O3
CAS No. 1207360-89-1 SDF Download GDC-0349 SDF
Smiles CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4COC4)C(=N2)N5CCOCC5C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 91 mg/mL ( (201.08 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble


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In vivo
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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.

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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

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