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GDC-0349

CAS No. : 1207360-89-1

MCE 站：GDC-0349

产品活性：GDC-0349 是一种有效的，ATP竞争性的选择性 mTOR 抑制剂，K_i 值为 3.8 nM。GDC-0349 抑制 mTORC1 和 mTORC2 复合体。

研究领域：PI3K/Akt/mTOR  |  Autophagy

作用靶点：mTOR  |  Autophagy

In Vitro: GDC-0349 (Compound 8h) is a remarkably selective mTOR inhibitor, with less than 25% inhibition of 266 kinases, including all isoforms of PI3K when tested at 1 μM.

In Vivo: When dosed orally once daily in athymic mice in a MCF7-neo/Her2 tumor xenograft model (PI3K mutation), GDC-0349 (Compound 8h) inhibits tumor growth in a dose-dependent manner, achieving stasis (99% TGI) at the maximum tolerated dose. Body weight change is less than 10% up to the highest dose. GDC-0349 is also efficacious in other xenograft models, including PC3 (PTEN null) and 786-0 (VHL mutant). Similar levels of tumor growth inhibition are achieved when GDC-0349 is administered once every three days at higher doses compared to once every day. GDC-0349 has ~10-fold reduced free plasma clearance in both mice (100 mL/min/kg) and rats (171 mL/min/kg in rat).

相关产品：Covalent Screening Library Plus  |  Clinical Compound Library Plus  |  Bioactive Compound Library Plus  |  Kinase Inhibitor Library  |  PI3K/Akt/mTOR Compound Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Clinical Compound Library  |  Autophagy Compound Library  |  Anti-Aging Compound Library  |  Covalent Screening Library  |  Antioxidants Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Oxygen Sensing Compound Library  |  Glycolysis Compound Library  |  Cytoskeleton Compound Library  |  Glutamine Metabolism Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Lung Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  Rapamycin  |  Everolimus  |  MHY1485  |  3BDO  |  Temsirolimus  |  Salidroside  |  Torkinib  |  PI-103  |  D-α-Hydroxyglutaric acid disodium  |  L-Leucine  |  Dihydromyricetin  |  PKI-402  |  Polyphyllin I  |  Rheb inhibitor NR1  |  GSK1059615  |  GNE-317  |  PP121  |  WYE-354  |  Cyclovirobuxine D  |  HDACs/mTOR Inhibitor 1  |  XL388  |  ETP-46464  |  Palomid 529  |  WAY-600  |  Arnicolide D  |  (+)-Usnic acid  |  hSMG-1 inhibitor 11j  |  mTOR inhibitor-1  |  TMBIM6 antagonist-1  |  Hederacolchiside A1

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