Home PI3K/Akt/mTOR mTOR inhibitor GDC-0349

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GDC-0349 mTOR inhibitor

Cat.No.S8040

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 mTOR inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 452.55

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Quality Control

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

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (201.08 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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In vivo
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Chemical Information, Storage & Stability

Molecular Weight 452.55 Formula

C24H32N6O3

 Storage (From the date of receipt)
CAS No. 1207360-89-1 Download SDF Storage of Stock Solutions

Synonyms RG-7603 Smiles CCNC(=O)NC1=CC=C(C=C1)C2=NC3=C(CCN(C3)C4COC4)C(=N2)N5CCOCC5C

Mechanism of Action

Targets/IC50/Ki
mTOR
3.8 nM(Ki)
PI3Kα
~3 μM(Ki)
In vitro
GDC-0349 has remarkable selectivity over 266 kinases, including all isoforms of PI3K. This compound 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.
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), this compound 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).
References

Applications

Methods Biomarkers Images PMID
Western blot p-AKT / AKT1 / p-S6K / S6K1 / LC3B-II / ATG-7 / Beclin-1 / p62
S8040-WB1
27291151

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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