An EZH2 inhibitor
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PF-06726304

Item No. 44260

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,8-dichloro-2-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-7-(3,5-dimethyl-4-isoxazolyl)-3,4-dihydro-1(2H)-isoquinolinone
CAS Number
1616287-82-1
Molecular Formula
C22H21Cl2N3O3
Formula Weight
446.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
O=C(C1=C(C(C2=C(ON=C2C)C)=CC(Cl)=C1CC3)Cl)N3CC4=C(C=C(NC4=O)C)C
InChi Code
InChI=1S/C22H21Cl2N3O3/c1-10-7-11(2)25-21(28)16(10)9-27-6-5-14-17(23)8-15(20(24)19(14)22(27)29)18-12(3)26-30-13(18)4/h7-8H,5-6,9H2,1-4H3,(H,25,28)
InChi Key
PDKDOPJQPKXNCT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $39

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    5 mg

    $97

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    10 mg

    $174

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    25 mg

    $385

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    Product Description

    PF-06726304 is an inhibitor of enhancer of zeste homolog 2 (EZH2; Ki = 0.7 nM).1 In vivo, PF-06726304 (200 and 300 mg/kg) reduces tumor volume and intratumor histone methylation in a Karpas-422 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kung, P.P., Rui, E., Bergqvist, S., et al. Design and synthesis of pyridone-containing 3,4-dihydroisoquinoline-1(2H)-ones as a novel class of enhancer of zeste homolog 2 (EZH2) inhibitors. J. Med. Chem. 59(18), 8306-8325 (2016).