An EZH2 inhibitor
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PF-06821497

Item No. 42500

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5,8-dichloro-2-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-3,4-dihydro-7-[(R)-methoxy-3-oxetanylmethyl]-1(2H)-isoquinolinone
CAS Number
1844849-10-0
Synonyms
  • Mevrometostat
Molecular Formula
C22H24Cl2N2O5
Formula Weight
467.3
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Slightly Soluble: 0.1-1 mg/mlWater: Slightly Soluble: 0.1-1 mg/ml
SMILES
COC(C=C(NC1=O)C)=C1CN(CCC2=C(Cl)C=C3[C@@H](C4COC4)OC)C(C2=C3Cl)=O
InChi Code
InChI=1S/C22H24Cl2N2O5/c1-11-6-17(29-2)15(21(27)25-11)8-26-5-4-13-16(23)7-14(19(24)18(13)22(26)28)20(30-3)12-9-31-10-12/h6-7,12,20H,4-5,8-10H2,1-3H3,(H,25,27)/t20-/m1/s1
InChi Key
RXCVUHMIWHRLDF-HXUWFJFHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

    $488

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    25 mg

    $731

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    Product Description

    PF-06821497 is an enhancer of zeste homolog 2 (EZH2) inhibitor (Ki = <0.1 nM for EZH2Y641N).1 It is selective for EZH2 over a panel of 14 methyltransferases, 40 kinases, and 79 additional targets at 10 µM but does bind to EZH1 (Ki = 70 nM). PF-06821497 reduces trimethylation of lysine 27 on histone H3 (H3K27Me3) in, and the proliferation of, Karpas-422 non-Hodgkin lymphoma cells, which endogenously express EZH2Y641N (IC50s = 4 and 6 nM, respectively). In vivo, PF-06821497 (100 mg/kg, s.c.) induces tumor regression 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., Bingham, P., Brooun, A., et al. Optimization of orally bioavailable enhancer of zeste homolog 2 (EZH2) inhibitors using ligand and property-based design strategies: Identification of development candidate (R)-5,8-dichloro-7-(methoxy(oxetan-3-yl)methyl)-2-((4-methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3,4-dihydroisoquinolin-1(2H)-one (PF-06821497). J. Med. Chem. 61(3), 650-665 (2018).