PFI-1 (PF-6405761) 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 in a cell-free assay.

Price Stock Quantity  
USD 200 In stock
USD 60 In stock
USD 470 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

PFI-1 (PF-6405761) Chemical Structure

PFI-1 (PF-6405761) Chemical Structure
Molecular Weight: 347.39

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

PFI-1 (PF-6405761) is available in the following compound libraries:

Epigenetic Reader Domain Inhibitors with Unique Features

  • Pan BET Inhibitor

    Bromosporine Pan-BET inhibitor, BRD2, IC50=0.41 μM; BRD4, IC50=0.29 μM; BRD9, IC50=0.122 μM; CECR2, IC50=0.017 μM.

  • Most Potent BET Inhibitor

    I-BET-762 BET proteins, IC50=~35 nM.

  • BET Inhibitor in Clinical Trial

    RVX-208 Phase II for Dyslipidemia.

  • Newest BET Inhibitor

    Bromosporine Broad spectrum inhibitor for bromodomains with IC50 of 0.41 μM, 0.29 μM, 0.122 μM and 0.017 μM for BRD2, BRD4, BRD9 and CECR2, respectively.

Product Information

  • Compare Epigenetic Reader Domain Inhibitors
    Compare Epigenetic Reader Domain Products
  • Research Area

Product Description

Biological Activity

Description PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.
Targets BRD4 [1]
(Cell-free assay)
IC50 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(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
Formulation Saline
Dosages 1 mg/kg
Administration Intravenous injection

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Fish PV, et al. J Med Chem, 2012, 55(22), 9831-9837.

[2] Cheng Z, et al. Clin Cancer Res, 2013, 19(7), 1-12.

view more

Chemical Information

Download PFI-1 (PF-6405761) SDF
Molecular Weight (MW) 347.39


CAS No. 1403764-72-6
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 69 mg/mL (198.62 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
* <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)-

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Epigenetic Reader Domain Products

Recently Viewed Items

Tags: buy PFI-1 (PF-6405761) | PFI-1 (PF-6405761) supplier | purchase PFI-1 (PF-6405761) | PFI-1 (PF-6405761) cost | PFI-1 (PF-6405761) manufacturer | order PFI-1 (PF-6405761) | PFI-1 (PF-6405761) distributor
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us