PFI-1 - Names and Identifiers
PFI-1 - Physico-chemical Properties
Molecular Formula | C16H17N3O4S
|
Molar Mass | 347.39 |
Solubility | DMSO: ≥10mg/mL |
Appearance | powder |
Color | white to beige |
Storage Condition | Sealed in dry,2-8°C |
MDL | MFCD22580416 |
Use | PFI-1 |
In vitro study | PFI-1 binds to the cAMP response binding element binding protein with a K D of 49 μm. PFI-1 inhibition of IL-6 production from LPS-stimulated human blood mononuclear cells, the EC50 was 1.89 μm. PFI-1 action on T4302 CD133 PFI-1 inhibit the proliferation of three NET cell lines (pancreatic NET-derived Bon-1, and lung NET-derived H727 and H720). |
In vivo study | PFI-1 was administered intravenously to rats at a dose of 1 mg/kg with a volume of distribution of 1 L/kg and a plasma clearance of 18/mL • min. |
PFI-1 - Risk and Safety
PFI-1 - Preparation solution concentration reference
| 1mg | 5mg | 10mg |
---|
1 mM | 2.879 ml | 14.393 ml | 28.786 ml |
5 mM | 0.576 ml | 2.879 ml | 5.757 ml |
10 mM | 0.288 ml | 1.439 ml | 2.879 ml |
5 mM | 0.058 ml | 0.288 ml | 0.576 ml |
Last Update:2024-01-02 23:10:35
PFI-1 - Reference Information
biological activity | PFI-1 (PF-6405761) is a highly selective BET (Bromodomain-containing protein) inhibitor, the IC50 in the cell-free assay was 0.22 μm and 98 nM for BRD4 and BRD2, respectively. |
Target | Value |
BRD2
(Cell-free assay)
| 98 nM |
BRD4
(Cell-free assay)
| 0.22 μM |
Last Update:2024-04-09 02:00:14