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    PFI-1 (PF-6405761)
    PFI-1 (PF-6405761)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0413
    CAS #: 1403764-72-6Purity ≥98%

    Description: PFI-1 is a novel, highly potent and selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in cell-free assays. Co-crystal structures showed that PFI-1 acts as an acetyl-lysine (Kac) mimetic inhibitor efficiently occupying the Kac binding site in BRD4 and BRD2. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. PFI-1 has antiproliferative effects on leukaemic cell lines and efficiently abrogates their clonogenic growth. Exposure of sensitive cell lines with PFI-1 results in G1 cell cycle arrest, down-regulation of MYC expression as well as induction of apoptosis and induces differentiation of primary leukaemic blasts.

    References: J Med Chem. 2012 Nov 26;55(22):9831-7; Clin Cancer Res. 2013 Apr 1;19(7):1748-59. 

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    Molecular Weight (MW)347.39
    FormulaC16H17N3O4S
    CAS No.1403764-72-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 69 mg/mL (198.6 mM)
    Water: <1 mg/mL
    Ethanol:  <1 mg/mL
    Other info

    Chemical Name: 2-methoxy-N-(3-methyl-2-oxo-1,2,3,4-tetrahydroquinazolin-6-yl)benzenesulfonamide

    InChi Key: TXZPMHLMPKIUGK-UHFFFAOYSA-N

    InChi Code: InChI=1S/C16H17N3O4S/c1-19-10-11-9-12(7-8-13(11)17-16(19)20)18-24(21,22)15-6-4-3-5-14(15)23-2/h3-9,18H,10H2,1-2H3,(H,17,20)

    SMILES Code: O=S(C1=CC=CC=C1OC)(NC2=CC3=C(NC(N(C)C3)=O)C=C2)=O

    SynonymsPFI 1; PFI-1; PFI1


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    In Vitro

    In vitro activity: 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. PFI-1 induces dose-dependent reduction of cell viability in T4302 CD133+ cells. 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).


    Kinase Assay: PFI-1 is a selective BET (bromodomain-containing protein) inhibitor for BRD4 with IC50 of 0.22 μM in a cell-free assay.


    Cell Assay: 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.

    In VivoPFI-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.
    Animal modelRats model
    Formulation & DosageDissolved in normal saline; 1mg/kg;  i.v. injection
    References

    J Med Chem. 2012 Nov 26;55(22):9831-7; Clin Cancer Res. 2013 Apr 1;19(7):1748-59. 


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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