A potent EZH2 inhibitor
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CPI-1205

Item No. 22962

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-[1-(2,2,2-trifluoroethyl)-4-piperidinyl]ethyl]-1H-indole-3-carboxamide
CAS Number
1621862-70-1
Synonyms
  • ​Lirametostat
Molecular Formula
C27H33F3N4O3
Formula Weight
518.6
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 33 mg/mlDMF:PBS (pH 7.2) (1:5): 0.16 mg/mlDMSO: 20 mg/mlEthanol: 2 mg/ml
λmax
213, 293 nm
SMILES
CC(N1)=CC(OC)=C(CNC(C2=C(C)N([C@H](C)C3CCN(CC(F)(F)F)CC3)C4=C2C=CC=C4)=O)C1=O
InChi Code
InChI=1S/C27H33F3N4O3/c1-16-13-23(37-4)21(25(35)32-16)14-31-26(36)24-18(3)34(22-8-6-5-7-20(22)24)17(2)19-9-11-33(12-10-19)15-27(28,29)30/h5-8,13,17,19H,9-12,14-15H2,1-4H3,(H,31,36)(H,32,35)/t17-/m1/s1
InChi Key
HPODOLXTMDHLLC-QGZVFWFLSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    Product Description

    CPI-1205 is a potent and orally bioavailable inhibitor of the lysine methyltransferase EZH2 (IC50s = 2 and 3 nM for wild-type and the constitutively active EZH2 Y641N catalytic mutant, respectively).1 It is selective for EZH2 over a panel of 30 histone and DNA methyltransferases and 54 receptors, transporters, and ion channels at a concentration of 10 μM. However, CPI-1205 does inhibit EZH1 (IC50 = 52 nM). CPI-1205 decreases levels of H2K27me3 in HeLa cells (EC50 = 32 nM). In vivo, CPI-1205 (160 mg/kg) reduces tumor size and H3K27me3 levels in a KARPAS-422 B cell lymphoma xenograft mouse model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Baswani, R.G., Gehling, V.S., Dakin, L.A., et al. Identification of (R)-N-((4-Methoxy-6-methyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-2-methyl-1-(1-(1-(2,2,2-trifluoroethyl)piperidin-4-yl)ethyl)-1H-indole-3-carboxamide (CPI-1205), a potent and selective inhibitor of histone methyltransferase EZH2, suitable for phase I clinical trials for B-cell lymphomas. J. Med. Chem. 59(21), 9928-9941 (2016).