CPI-360

SKU: orb1685548

Description

CPI-360 is a potent and selective small molecule inhibitor of EZH2, demonstrating sub-nanomolar enzymatic inhibition and cellular activity. It has shown antitumor efficacy in EZH2-dependent xenograft models, supporting its use as a chemical probe for epigenetic research in oncology, both in vitro and in vivo.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1802175-06-9
• MW: 437.53
• Purity: 99.52% (May vary between batches)
• Formula: C₂₅H₃₁N₃O₄
• SMILES: [C@H](C)(N1C=2C(C(C(NCC3=C(OC)C=C(C)NC3=O)=O)=C1C)=CC=CC2)C4CCOCC4
• Target: Histone Methyltransferase,Apoptosis
• Solubility: H2O:< 1 mg/mL (insoluble or slightly soluble);DMF:9 mg/mL (20.57 mM);Ethanol:27 mg/mL (61.71 mM);DMSO:22.5 mg/mL (51.43 mM)

Bioactivity

• Target IC50:
  EZH1:102.3 nM
• In Vivo:
  In mice bearing KARPAS-422 xenografts, CPI-360 (200 mg/kg, s.c.) reduces tumor growth by 44%.
• In Vitro:
  In KARPAS-422 cells, CPI-360 potently reduces global H3K27me3 and H3K27me2 levels with EC50 of 56 nM and 65 nM, respectively. CPI-360 also causes time-dependent transcriptional changes, and affects the viability of Y641N mutant EZH2-containing KARPAS-422 cells. In addition, CPI-360 gradually arrests KARPAS-422 cells in the G1 cell cycle stage followed by the induction of apoptosis.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Synonym 2, Synonym 2, Histone Methyltransferase, HistoneMethyltransferase, EZH2, CPI 360, CPI360, CPI-360, Apoptosis

Compound Identifiers

PubChem CID

73442743