Antibodies
PFI-1 (PF-06405761)
- 貨號 Cat. No.
- S1216
- 規格 Size
- 5~200mg
- 品牌 Brand
- Selleckchem
Description
PFI-1 (PF-06405761)Licensed and Manufactured by Pfizer
Catalog No.S1216
PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM.
| Size | Price | Stock | Quantity | ||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| |||||||||||||||
Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
Biological Activity
| Description | PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM. | |||||
|---|---|---|---|---|---|---|
| Targets | BRD4 | |||||
| IC50 | 0.22 μM [1] | |||||
| In vitro | PFI-1 binds to with cyclic AMP response binding protein with KD of 49 μM. PFI-1 has an EC50 of 1.89 μM for the inhibition of IL6 production from human blood mononuclear cells stimulated by LPS. [1] PFI-1 induces dose-dependent reduction of cell viability in T4302 CD133+ cells. [2] PFI-1 inhibits the proliferating of three NET cell lines (Bon-1 derived from a pancreatic NET, and H727 and H720 derived from lung NETs). [3] | |||||
| In vivo | PFI-1 administrated (1 mg/kg i.v.) in the rat results in the volume of distribution of 1 L/kg, the plasma clearance of 18/mL·min–1·kg–1 and half-life of 1 hour. PFI-1 oral dosed (2 mg/kg) in the rat results in the oral bioavailability as low as 32%. PFI-1 administrated (2 mg/kg s.c.) in the mouse results in a Cmax of 58 ng/mL with a Tmax of 1 h and a half-life of approximately 2 hours. [1] | |||||
| Features | ||||||
Protocol(Only for Reference)
Cell Assay: [2]
| Cell lines | T4302 CD133+ cells |
|---|---|
| Concentrations | 1 mM |
| Incubation Time | 5 days |
| Method | To determine dose response, cells are aliquoted into 96-well plate at 5 × 103 cells per well in triplicates. PFI-1 is added by 2- or 4-fold serial dilutions. Cell number is measured 5 days after plating using the CellTiter-Glo Kit and normalized to corresponding vehicle-treated groups. IC50 values are calculated by the GraphPad Prism 5 software using the 4-parameter logistic nonlinear regression model. To calculate the relative growth of cells, averaged cell titers of each group on day 1 are assigned a value of 1. All subsequent cell titer values are normalized accordingly. |
Animal Study: [1]
| Animal Models | Rats |
|---|---|
| Dosages | 1 mg/kg |
| Administration | Intravenous injection |
References
Chemical Information
Download PFI-1 (PF-06405761) SDF
| Molecular Weight (MW) | 347.39 |
|---|---|
| Formula | C16H17N3O4S |
| CAS No. | 1403764-72-6 |
| Storage | 3 years -20℃Powder |
|---|---|
| 6 months-80℃in DMSO | |
| Syonnyms | N/A |
| Solubility (25°C) * | In vitro | DMSO | 69 mg/mL (198 mM) |
|---|---|---|---|
| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| * <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. | |||
| Chemical Name | Benzenesulfonamide, 2-methoxy-N-(1,2,3,4-tetrahydro-3-methyl-2-oxo-6-quinazolinyl)- |
|---|
Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
|---|---|---|---|---|
| Mass(mg) | 0.34739 | 3.4739 | 6.9478 | 10.4217 |
