[CAS NO. 1616287-82-1]  PF-06726304

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PRODUCTS SPECIFICATIONS [1616287-82-1]

Catalog
SLK-S8494
Brand
Selleck
CAS
1616287-82-1

DESCRIPTION [1616287-82-1]

Overview

MDL-
Molecular Weight446.33
Molecular FormulaC22H21Cl2N3O3
SMILESO=C1N(CC2=C(C)C=C(C)NC2=O)CCC3=C1C(Cl)=C(C4=C(C)ON=C4C)C=C3Cl

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

1 mg5 mg10 mg
1 mM2.2405 mL11.2025 mL22.4049 mL
5 mM0.4481 mL2.2405 mL4.4810 mL
10 mM0.2240 mL1.1202 mL2.2405 mL
50 mM---

Description

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

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.