Name | GDC-0349 |
Synonyms | CS-695 RG-7603 GDC-0349 (S)-1-Ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimi (S)-1-ethyl-3-(4-(4-(3-methylmorpholino)-7-(oxetan-3-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-2-yl)phenyl)urea N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea Urea, N-ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]- GDC-0349 N-Ethyl-N'-[4-[5,6,7,8-tetrahydro-4-[(3S)-3-methyl-4-morpholinyl]-7-(3-oxetanyl)pyrido[3,4-d]pyrimidin-2-yl]phenyl]urea |
CAS | 1207360-89-1 |
EINECS | 200-258-5 |
Molecular Formula | C24H32N6O3 |
Molar Mass | 452.55 |
Density | 1.269 |
Storage Condition | -20℃ |
In vitro study | GDC-0349 is much more selective for mTOR than for the other 266 kinases and all PI3K subtypes. |
In vivo study | In the study of PK/PD in vivo, GDC-0349 treatment of mice inhibited downstream markers of mTOR, including phospho -4EBP1 and phospho-Akt(S473), this is consistent with inhibition of the mTORC1 and mTORC2 complexes. GDC-0349 treatment of mouse xenograft models can regulate signaling pathways in a dose-dependent manner. GDC-0349 oral administration of nude mice carrying MCF7-neo/Her2 xenograft model (PI3K mutant) once a day inhibited tumor growth in a dose-dependent manner. GDC-0349 is also effective in other xenograft models, including PC3(PTEN null) and 786-O(VHL mutant). |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.21 ml | 11.049 ml | 22.097 ml |
5 mM | 0.442 ml | 2.21 ml | 4.419 ml |
10 mM | 0.221 ml | 1.105 ml | 2.21 ml |
5 mM | 0.044 ml | 0.221 ml | 0.442 ml |