A selective EZH2 inhibitor
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CPI-169

Item No. 18299

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]-1-[1-[1-(ethylsulfonyl)-4-piperidinyl]ethyl]-2-methyl-1H-indole-3-carboxamide
CAS Number
1450655-76-1
Molecular Formula
C27H36N4O5S
Formula Weight
528.7
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 25 mg/mLDMF:PBS(pH 7.2)(1:1): 0.5 mg/mLDMSO: 20 mg/mLEthanol: 10 mg/mL
λmax
291 nm
SMILES
CC(NC1=O)=CC(OC)=C1CNC(C2=C(C)N(C(C)C3CCN(S(CC)(=O)=O)CC3)C4=C2C=CC=C4)=O
InChi Code
InChI=1S/C27H36N4O5S/c1-6-37(34,35)30-13-11-20(12-14-30)18(3)31-19(4)25(21-9-7-8-10-23(21)31)27(33)28-16-22-24(36-5)15-17(2)29-26(22)32/h7-10,15,18,20H,6,11-14,16H2,1-5H3,(H,28,33)(H,29,32)
InChi Key
LHGUZCKPFXXVPV-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $75

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    5 mg

    $259

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    Cayman Chemical
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    Product Description

    CPI-169 is a selective EZH2 inhibitor with IC50 values of 0.24, 0.51, and 6.1 nM for wild-type EZH2, Y641N mutant EZH2, and wild-type EZH1, respectively.1 It decreases cellular levels of H3K27me3 (EC50 = 70 nM), triggering cell cycle arrest and ultimately resulting in apoptosis in a large panel of non-Hodgkin’s lymphoma (NHL) cell lines.1 With subcutaneous administration of 200 mg/kg/twice a day, CPI-169 was shown to inhibit tumor growth in a NHL xenograft model, reducing global H3K27me3.1 It has also been shown to synergize with the B-cell lymphoma 2 inhibitor, ABT-199 (Item No. 16233), to suppress the growth of NHL cell lines.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).