A selective EZH2 inhibitor
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CPI-360

Item No. 19125

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-[(1,2-dihydro-4-methoxy-6-methyl-2-oxo-3-pyridinyl)methyl]-2-methyl-1-[(1R)-1-(tetrahydro-2H-pyran-4-yl)ethyl]-1H-indole-3-carboxamide
CAS Number
1802175-06-9
Molecular Formula
C25H31N3O4
Formula Weight
437.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 10 mg/mlDMSO: 25 mg/mlEthanol: 30 mg/mlEthanol:PBS (pH7.2) (1:7): 0.12 mg/ml
λmax
212, 292 nm
SMILES
CC(N1)=CC(OC)=C(CNC(C2=C(C)N([C@H](C)C3CCOCC3)C4=C2C=CC=C4)=O)C1=O
InChi Code
InChI=1S/C25H31N3O4/c1-15-13-22(31-4)20(24(29)27-15)14-26-25(30)23-17(3)28(21-8-6-5-7-19(21)23)16(2)18-9-11-32-12-10-18/h5-8,13,16,18H,9-12,14H2,1-4H3,(H,26,30)(H,27,29)/t16-/m1/s1
InChi Key
PFPSFENQCNMITC-MRXNPFEDSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    500 µg

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    1 mg

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    5 mg

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    10 mg

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    Cayman Chemical
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    Product Description

    CPI-360 is a selective EZH2 inhibitor with IC50 values of 0.5 and 2.5 nM for wild-type EZH2 and Y641N mutant EZH2, respectively.1 It decreases cellular levels of H3K27me3 and H3K27me2 (EC50s = 56 and 65 nM, respectively), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin’s lymphoma (NHL) cell lines.1 Twice daily, subcutaneous administration of 200 mg/kg of CPI-360 reduced tumor growth of KARPAS-422 xenografts in mice.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Bradley, W.D., Arora, S., Busby, J., et al. EZH2 inhibitor efficacy in non-Hodgkin’s lymphoma does not require suppression of H3K27 monomethylation. Chem. Biol. 21, 1-13 (2014).