CPI203

SKU: orb1305480

Description

CPI203

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 202591-23-9
• MW: 399.9
• Purity: 99.71% (May vary between batches)
• Formula: C₁₉H₁₈ClN₅OS
• SMILES: CC=1C2=C(N3C(C(CC(N)=O)N=C2C4=CC=C(Cl)C=C4)=NN=C3C)SC1C
• Target: Epigenetic Reader Domain
• Solubility: DMSO:200 mM

Bioactivity

• Target IC50:
  BET BD:37 nM
• In Vitro:
  CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib.
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• Cell Research:
  MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203. MTT is added for 2-6 additional hours before spectrophotometric measurement. Each measurement is made in triplicate. Values are represented using untreated control cells. The GI50 is calculated as the concentration that produced 50 % growth inhibition. Combination indexes (CIs) are calculated by using the Calcusyn software version 2.0. The interaction between two drugs is considered synergistic when CI <1. (Only for Reference)
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Storage & Handling

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

Alternative Names

CPI-203, CPI203, CPI 203, BRD4, Epigenetic Reader Domain, EpigeneticReaderDomain

Compound Identifiers

PubChem CID

19704953