Pifusertib, also known as TAS-117, is a PKB/Akt inhibitor potentially for the treatment of solid tumors. TAS-117 induced significant growth inhibition, associated with downregulation of phosphorylated Akt (p-Akt), selectively in MM cell lines with high baseline p-Akt. TAS-117 induced significant cytotoxicity in MM cells even in the presence of BM stromal cells, associated with inhibition of IL6 secretion. TAS-117 significantly inhibited human MM cell growth in murine xenograft models. TAS-117 triggered apoptosis and autophagy, as well as induction of endoplasmic reticulum (ER) stress response with minimal expression of C/EBP homologous protein (CHOP), a fatal ER stress marker. TAS-117 enhanced bortezomib-induced cytotoxicity in vivo, associated with prolonged host survival.
MedKoo Cat#: 527005
Name: Pifusertib
CAS#: 1402602-94-1
Chemical Formula: C26H24N4O2
Exact Mass: 424.1899
Molecular Weight: 424.50
Elemental Analysis: C, 73.56; H, 5.70; N, 13.20; O, 7.54
The following data is based on the product molecular weight 424.50 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
