GDC-0349 is an ATP-competitive, potent and selective inhibitor of mTOR with an Ki value of 3.8 nM. It has ~800-fold selectivity over PI3Ka and in PC3 cells exhibits an EC50 of 270 nM. Additionally GDC-0349 showed less than 25% inhibition in a panel of 266 kinases, including all isoforms of PI3K. In in vivo PK/PD mouse studies, GDC-0349 inhibits key mTOR biomarkers such as phospho-4EBP1 and phospho-Akt (S473), which supports the notion of concurrent inhibition of both mTORC1 and mTORC2 complexes. (1)
Technical information:
| Chemical Formula: | C24H32N6O3 | |
| CAS #: | 1207360-89-1 | |
| Molecular Weight: | 452.55 | |
| Purity: | > 98% | |
| Appearance: | light yellow | |
| Chemical Name: | (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 | |
| Solubility: | Up to 50 mM in DMSO | |
| Synonyms: | GDC-0349, GDC 0349, GDC0349, RG7603 |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
| 1. | Pei et al., Discovery and Biological Profiling of Potent and Selective mTOR Inhibitor GDC-0349. ACS Med. Chem. Lett. 2013, 4, 103-107. |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.
