1. Epigenetics
  2. Histone Methyltransferase
  3. PF-06726304

PF-06726304 

Cat. No.: HY-103682 Purity: 98.96%
Handling Instructions

PF-06726304 is a potent and selective EZH2 inhibitor with a Ki of 0.7 nM.

For research use only. We do not sell to patients.

PF-06726304 Chemical Structure

PF-06726304 Chemical Structure

CAS No. : 1616287-82-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 101 In-stock
Estimated Time of Arrival: December 31
5 mg USD 92 In-stock
Estimated Time of Arrival: December 31
10 mg USD 156 In-stock
Estimated Time of Arrival: December 31
25 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 660 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

PF-06726304 is a potent and selective EZH2 inhibitor with a Ki of 0.7 nM.

IC50 & Target

Ki: 0.7 nM (EZH2)[1]

In Vitro

PF-06726304 displays potent biochemical and cellular potencies in the Karpas-422 cell line. Upon treatment with PF-06726304 for 7 days, both TNFRSF21 and PRDM1 are upregulated in Karpas-422 cells containing both wild-type and Y641N mutant EZH2 proteins in a dose-dependent manner[1].

In Vivo

PF-06726304 inhibits tumor growth and induces robust modulation of downstream biomarkers in a Karpas-422 in vivo model. Treatment with PF-06726304 is well-tolerated at 200 and 300 mg/kg in mice, with less than 10% body weight loss observed during the course of the experiment. on day 20, PF-06726304 demonstrates tumor stasis and regression at the 200 and 300 mg/kg dose levels, respectively. In addition, tumor growth inhibition is sustained for at least another 3 weeks after the last dose, demonstrating the ability of PF-06726304 to mediate long-term epigenetic reprogramming in cells. PF-06726304 induces approximately 55.5% and 66.4% reduction of the H3K27Me3 level at doses of 200 and 300 mg/kg, respectively. In addition, the PRC2 target genes TNFRSF21 and PRDM1 are both strongly upregulated in both the 200 and 300 mg/kg dosing arms[1].

Molecular Weight

446.33

Formula

C₂₂H₂₁Cl₂N₃O₃

CAS No.

1616287-82-1

SMILES

O=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl

Shipping

Room temperature in continental US; may vary elsewhere

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 15 mg/mL (33.61 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2405 mL 11.2025 mL 22.4049 mL
5 mM 0.4481 mL 2.2405 mL 4.4810 mL
10 mM 0.2240 mL 1.1202 mL 2.2405 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

PF-06726304 dilutions are prepared. Karpas-422 cells are treated with PF-06726304. Cell Growth Inhibition is performed and IC50 values are calculated[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Mice: Mice are treated with PF-06726304 at 200 and 300 mg/kg BID for 20 days. Tumor growth is monitored for several weeks following cessation of dosing. Average body weight is measured during the duration of compound treatment. Global H3K27Me3 levels are measured in Karpas-422 tumors harvested on day 20[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
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PF-06726304
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HY-103682
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