PF-06726304

Catalog No.S8494 Synonyms: PF-6726304

PF-06726304 Chemical Structure

Molecular Weight(MW): 446.33

PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.

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Biological Activity

Description PF-06726304 is a selective EZH2 inhibitor with Ki values of 0.7 nM and 3 nM for WT EZH2 and Y641N respectively; also inhibits H3K27me3 with the IC50 value of 15 nM.
Targets
Ezh2 (wild-type) [1]
(cell-free)
EZH2 Y641N [1]
(cell-free)
0.7 nM(Ki) 3 nM(Ki)
In vitro

PF-06726304 displays very potent EZH2 biochemical inhibition as well as good activity in the cell H3K27Me3 reduction and antiproliferation effect[1].

In vivo PF-06726304 displays robust in vivo antitumor growth activity and dose-dependent de-repression of EZH2 target genes. PF-06726304 displays good efficacy in a diffuse large B-cell lymphoma Karpas-422 tumor model and exhibited on-target pharmacodynamic effects in vivo[1].

Protocol

Cell Research:

[1]

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  • Cell lines: Karpas-422 cell line
  • Concentrations: --
  • Incubation Time: 72 h
  • Method:

    Karpas-422 cells are plated in complete cell culture medium (100 μL/well) in a 96-well clear, V bottom polystyrene cell culture plate at a density of 2500 cells/well. The cells are then incubated for 2−3 h at 37 °C and 5% CO2. Compound dilution plates are prepared in 96-well clear, U-bottom polypropylene plates in 100% DMSO at 10 mM stock concentration in duplicate wells using an 11-point serial dilution (1:3 dilutions). Compounds are further diluted in growth medium, and 25 μL is added to each well of the cell plates. The highest compound concentration tested is 50 μM final, with a 0.5% final DMSO concentration. The plates are then incubated for 72 h at 37 °C and 5% CO2. At the end of the incubation period with compound, the plates are centrifuged at 2000 rpm for 5 min at room
    temperature, and the medium is removed. Then 100 μL of acid-extracted solution is added to each well. The plates are shaken for 50 min at 4 °C to lyse the cells, and then 38 μL of neutralization buffer is added. The plates are then frozen at −80 °C. The next day, the plates are shaken at room temperature to thaw. Cell lysates (50 μL/well) are then transferred to ELISA plates. The plates are covered and incubated for 2.5 h at room temperature with constant slow-speed shaking. After incubation, the plates are washed seven times (300 μL/well) with 1× wash buffer. Then 100 μL of biotinylated trimethylhistone H3K27 detection antibody is added to each well and incubated for 2 h at room temperature with constant slow-speed shaking. After incubation, the plates are washed as described above. Horseradish peroxidase-linked antibody (100 μL) is added to each well and incubated for 60 min at room temperature with constant slow-speed shaking. After incubation, the plates are
    washed. Finally, 100 μL of TMB substrate reagent is added to each well and incubated for 5 min at room temperature in the dark with slow shaking, after which 100 μL of stop solution is added to stop the reaction.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: Female Scid beige mice
  • Formulation: 0.5% NaCMC and 0.1% Tween 80 at a final pH of 4.5
  • Dosages: 30, 100, 300 mg/kg
  • Administration: oral
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 22 mg/mL (49.29 mM)
DMSO 10 mg/mL (22.4 mM)
Water 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 Information

Molecular Weight 446.33
Formula

C22H21Cl2N3O3

CAS No. 1616287-82-1
Storage powder
in solvent
Synonyms PF-6726304

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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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Related Antibodies

Histone Methyltransferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID