For research use only.
Catalog No.S8040 Synonyms: RG-7603
CAS No. 1207360-89-1
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.
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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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Choose Selective mTOR Inhibitors
|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.|
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. 
|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). |
|Animal Research: ||
|In vitro||DMSO||91 mg/mL (201.08 mM)|
|Ethanol||6 mg/mL (13.25 mM)|
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In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
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.
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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|
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.
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