An orally bioavailable EZH2 inhibitor
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EPZ011989

Item No. 19161

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,2-dihydro-4,6-dimethyl-2-oxo-3-pyridinyl)methyl]-3-[ethyl[trans-4-[(2-methoxyethyl)methylamino]cyclohexyl]amino]-2-methyl-5-[3-(4-morpholinyl)-1-propyn-1-yl]-benzamide
CAS Number
1598383-40-4
Molecular Formula
C35H51N5O4
Formula Weight
605.8
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 10 mg/mlEthanol: 20 mg/mlEthanol:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
244, 303 nm
SMILES
CN(CCOC)[C@@H]1CC[C@@H](N(C2=CC(C#CCN3CCOCC3)=CC(C(NCC4=C(C)C=C(C)NC4=O)=O)=C2C)CC)CC1
InChi Code
InChI=1S/C35H51N5O4/c1-7-40(30-12-10-29(11-13-30)38(5)15-18-43-6)33-23-28(9-8-14-39-16-19-44-20-17-39)22-31(27(33)4)34(41)36-24-32-25(2)21-26(3)37-35(32)42/h21-23,29-30H,7,10-20,24H2,1-6H3,(H,36,41)(H,37,42)/t29-,30-
InChi Key
XQFINGFCBFHOPE-WXUXXXNLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

    $132

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    1 mg

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    5 mg

    $1,048

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    Cayman Chemical
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    Product Description

    The lysine methyltransferase EZH2 (KMT6), part of polycomb repressive complex 2, catalyzes trimethylation of lysine 27 on histone H3 and is involved in proliferation and aggressive cell growth associated with neoplastic cells.1 EPZ011989 is an orally bioavailable EZH2 inhibitor with Ki values that are less than 3 nM for wild type and Tyr646 mutated EZH2.2 It displays 15-fold selectivity for EZH2 over EZH1 and is without effect against an array of other lysine methyltransferases.2 EPZ011989 demonstrates significant tumor growth inhibition in a mouse xenograft model of human B cell lymphoma.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Simon, J.A., and Lange, C.A. Roles of the EZH2 histone methyltransferase in cancer epigenetics. Mutat. Res. 647(1-2), 21-29 (2008).

    2. Campbell, J.E., Kuntz, K.W., Knutson, S.K., et al. EPZ011989, a potent, orally-available EZH2 inhibitor with robust in vivo activity. ACS Med. Chem. Lett. 6(5), 491-495 (2015).