Home Epigenetics Epigenetic Reader Domain inhibitor PFI-1 (PF-6405761)

PFI-1 (PF-6405761)

Licensed and Manufactured by Pfizer Catalog No.S1216

For research use only.

PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.

PFI-1 (PF-6405761) Chemical Structure

CAS No. 1403764-72-6

Selleck's PFI-1 (PF-6405761) has been cited by 7 Publications

Purity & Quality Control

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Biological Activity

Description PFI-1 (PF-6405761) is a highly selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM and for BRD2 with IC50 of 98 nM in a cell-free assay.
Targets
BRD2 [4]
(Cell-free assay)		 BRD4 [1]
(Cell-free assay)
98 nM 0.22 μM
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]

Protocol (from reference)

Cell Research:

[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 Research:

[1]
  • Animal Models: Rats
  • Dosages: 1 mg/kg
  • Administration: Intravenous injection

Solubility (25°C)

In vitro

 DMSO 69 mg/mL
(198.62 mM)
Water Insoluble
Ethanol Insoluble

Chemical Information

Molecular Weight 347.39
Formula

C16H17N3O4S
CAS No. 1403764-72-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1CC2=C(C=CC(=C2)NS(=O)(=O)C3=CC=CC=C3OC)NC1=O

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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