Description: |
GDC-0349 is a potent and selective ATP-competitive inhibitor of mTOR with Ki of 3.8 nM; >700-fold selectivity over PI3Kα and other 266 kinases.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. 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). For the detailed information of GDC-0349, the solubility of GDC-0349 in water, the solubility of GDC-0349 in DMSO, the solubility of GDC-0349 in PBS buffer, the animal experiment (test) of GDC-0349, the cell expriment (test) of GDC-0349, the in vivo, in vitro and clinical trial test of GDC-0349, the EC50, IC50,and affinity,of GDC-0349, For the detailed information of GDC-0349, the solubility of GDC-0349 in water, the solubility of GDC-0349 in DMSO, the solubility of GDC-0349 in PBS buffer, the animal experiment (test) of GDC-0349, the cell expriment (test) of GDC-0349, the in vivo, in vitro and clinical trial test of GDC-0349, the EC50, IC50,and affinity,of GDC-0349, Please contact DC Chemicals. |