GDC-0349

SKU: orb1685655

Description

GDC-0349

Research Area

Cell Biology, Signal Transduction

Key Properties

• CAS Number: 1207360-89-1
• MW: 452.55
• Purity: 98.98% (May vary between batches)
• Formula: C₂₄H₃₂N₆O₃
• SMILES: CCNC(=O)Nc1ccc(cc1)-c1nc2CN(CCc2c(n1)N1CCOC[C@@H]1C)C1COC1
• Target: Autophagy,mTOR,PI3K
• Solubility: DMSO:84 mg/mL (185.61 mM);10% DMSO+90% Saline:3.3 mg/mL (7.29 mM);Ethanol:6 mg/mL (13.26 mM);H2O:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

• Target IC50:
  mTOR:3.8 nM(Ki)
• 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).
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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Autophagy, Inhibitor, GDC 0349, GDC0349, GDC-0349, Mammalian target of Rapamycin, inhibit, mTOR, PI3Kα, RG 7603, RG7603, RG-7603

Compound Identifiers

PubChem CID

59239165