Home Epigenetics Histone Methyltransferase inhibitor - EZH1/2 inhibitor PF-06726304

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PF-06726304 Histone Methyltransferase inhibitor

Cat.No.S8494

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

Chemical Structure

Molecular Weight: 446.33

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S849401 Ethanol]22 mg/mL]false]DMSO]10 mg/mL]false]Water]Insoluble]false Purity: 99.02%
99.02

Chemical Information, Storage & Stability

Molecular Weight 446.33 Formula

C22H21Cl2N3O3

 Storage (From the date of receipt)
CAS No. 1616287-82-1 Download SDF Storage of Stock Solutions

Synonyms PF-6726304 Smiles CC1=CC(=C(C(=O)N1)CN2CCC3=C(C=C(C(=C3C2=O)Cl)C4=C(ON=C4C)C)Cl)C

Solubility

In vitro
Batch:

Ethanol : 22 mg/mL

DMSO : 10 mg/mL ( (22.4 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

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

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Ezh2 (wild-type) [1]
(cell-free)
0.7 nM(Ki)
EZH2 Y641N [1]
(cell-free)
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. This compound displays good efficacy in a diffuse large B-cell lymphoma Karpas-422 tumor model and exhibited on-target pharmacodynamic effects in vivo[1].
References

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