| Molecular Formula | C43H42N4O6
|
| Molar Mass | 710.82 |
| Appearance | Powder |
| Storage Condition | -20℃ |
| Use | S55746 (S 055746,BCL201) is a novel, orally active BCL-2 specific inhibitor with a Ki of 1.3 nM. It has a weak affinity for Bcl-XL, but not for MCL-1, BFL-1(BCL2A1/A1). |
| In vitro study | S55746 may occupy Bcl-2 of the hydrophobic grooves. In a series of blood cell lines, S55746 induces apoptotic markers such as phosphatidylserine externalization, caspase-3 activation and PARP fragmentation. RS4;11 cells were treated with S55746 for 72 hours, and S55746 was effective in inducing cell killing with an IC50 of 71.6 nM. In H146 cells (BCL-XL dependent cell line), its activity was greatly reduced with an IC50 of 1.7 μm. S55746 had no toxic effects on BCL-XL-dependent cells, such as platelets. |
| In vivo study | By oral route, mice were orally administered daily with S55746, S55746 had potent anti-tumor effects in two blood-transplanted tumor models (RS4;11 and Toledo), without causing weight loss and behavioral abnormalities. |
