217656
PI 3-K/mTOR Inhibitor III, PKI-179 (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, PI 3-K Inhibitor XVII, mTOR Inhibitor X)
Size
£566.00
- SKU:
- 217656
- Molecular Weight:
- 506.6
- Purity:
- ≥98% (HPLC)
- Storage Conditions:
- 4°C
- Supplier:
- United States Biological
- CAS Number:
- 1197160-28-3
- Format:
- Supplied as a white solid.
- Extra Details:
- 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)-Nʹ-4-pyridinylurea, hydrate CAS No: 1197160-28-3 Molecular Formula: C₂₅H₂₈N₈O₃•H₂O Solubility: DMSO Molecular Weight: 506.6 Purity: ≥98% (HPLC) Appearance: White solid Storage and Stability: May be stored at 4°C. For long-term storage, aliquot and store at 4°C. 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.
- Shipping Conditions:
- Blue Ice