| A cell-permeable triazinyl-phenyl-pyridinylurea compound that acts as a potent inhibitor against mTOR (IC50=0.42nM) and PI 3-K (IC50=8, 24, 74, 77, 14, and 11nM against isoform a, b, g,d, a E545K mutant, and a H1047R mutant, respectively) activities, exhibiting much reduced or little activity against a panel of 361 other kinases (IC50 >50uM), Cytochrome CYP isoforms, or hERG. It is reported to be orally available in mouse, rat, monkey, and dog species, and effectively suppress cancer growth both in cultures in vitro (IC50=22 and 29nM, respectively, against MDA361 and PC3mm2) and in mice in vivo (by 30% of control MDA361 tumor size on day 42, 50mg/kg/day p.o.) via apoptosis induction as a result of Akt/mTOR pathway inhibition. Synonyms: mTOR Inhibitor X, PI 3-K Inhibitor XVII, 1-(4-(4-(3-Oxa-8-azabicyclo[3.2.1]octan-8-yl)-6-morpholino-1,3,5-triazin-2-yl)-phenyl)-3-(pyridin-4-yl)urea, hydrate, N-(4-(4-(4-Morpholinyl)-6-(3-oxa-8-azabicyclo[3.2.1]oct-8-yl)-1,3,5-triazin-2-yl)phenyl)-N-4-pyridinylurea, hydrate CAS No: 1197160-28-3 Molecular Formula: C25H28N8O3H2O Solubility: DMSO Molecular Weight: 506.6 Purity: 98% (HPLC) Appearance: White solid Storage and Stability: May be stored at 4C. For long-term storage, aliquot and store at 4C. Do not freeze. For maximum recovery of product, centrifuge the original vial prior to removing the cap. Further dilutions can be made in assay buffer. |
