CPI-169 racemate

SKU: orb1300447

Description

CPI-169 is a highly potent and selective inhibitor of EZH2, demonstrating IC50 values of 0.24 nM for wild-type, 0.51 nM for the Y641N mutant, and 6.1 nM for EZH1. This compound is a valuable chemical probe for epigenetic research, enabling the study of histone methylation roles in cancer biology and other diseases in both cellular and animal models.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 1450655-76-1
• MW: 528.66
• Purity: 99.59% (May vary between batches)
• Formula: C₂₇H₃₆N₄O₅S
• SMILES: CCS(=O)(=O)N1CCC(CC1)C(C)n1c(C)c(C(=O)NCc2c(OC)cc(C)[nH]c2=O)c2ccccc12
• Target: Epigenetic Reader Domain,Histone Methyltransferase
• Solubility: Ethanol:93 mg/mL (175.92 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);DMSO:93 mg/mL (175.92 mM)

Bioactivity

• Target IC50:
  EZH1:6.1 nM|EZH2 (Y641N):0.51 nM|EZH2 (WT):0.24 nM
• In Vivo:
  In mice bearing KARPAS-422 xenografts, CPI-169 (200 mg/kg, s.c.) effectively suppresses H3K27me3 levels and results in lymphoma tumor regression without affecting body weight or causing any overt adverse effects.
• In Vitro:
  In KARPAS-422 cells, CPI-169 shows a dose-dependent inhibitory effect on cell viability, and produces synergy anti-proliferative activity when used in combination with ABT-199. In 16 out of 25 NHL cell lines, CPI-169 also suppresses cell growth with GI50 of <5 μM.
• Cell Research:
  Relative cell numbers are assessed by Cell Titer-Glo (CTG) luminescent cell viability assay using an Envision instrument. GraphPad Prism 6.0 is used for curve fitting, IC50/GI50 and Hill coefficient (H) calculations. The GI90 is calculated using the formula: EC90 = (90 /100-90)1/H * EC50.(Only for Reference)
• Animal Research:
  Animal Models: Mice bearing KARPAS-422 subcutaneous xenograftsFormulation: 10% DMSO + 60% polytheylene glycol 400 + 30% ddH2ODosages: 200 mg/kg, BIDAdministration: s.c.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

CPI 169, CPI 169 racemate, CPI169, CPI-169, CPI169 racemate, CPI-169 racemate, EZH1, EZH2 WT, EZH2 Y641N, Epigenetic Reader Domain, EpigeneticReaderDomain, Histone Methyltransferase, HistoneMethyltransferase

Compound Identifiers

PubChem CID

78357814