NEO2734

SKU: orb1219792

Description

NEO2734 is an orally active and selective inhibitor of p300/CBP and BET bromodomain(IC50 of <30 nM for both p300/CBP and BET bromodomains).NEO2734, a novel dual inhibitor of BET and CBP/p300, is active in both hotspot mutant (F133V) and non-hotspot mutant (Q165P) PCa cells in vitro and in vivo.

Key Properties

• CAS Number: 2081072-29-7
• MW: 435.44
• Purity: >98% (HPLC)
• Formula: C₂₂H₂₄F₃N₃O₃
• SMILES: Cc1cc(cn(C)c1=O)-c1ccc2nc(C3CCOCC3)n(CCOC(F)(F)F)c2c1
• Target: Epigenetic Reader Domain
• Solubility: In Vitro: DMSO : 100 mg/mL (229.65 mM)

Bioactivity

• In Vivo:
  Animal model: Mice (PER-403 and 14169 models). Dosage: 5, 8, 10 mg/kg. Administration: Orally, once daily for 28 days. Result: Two of the three mice treated with NEO2734 were alive by day 100.Provided markedly improved survival compared with EP, i-BET-762, and even iBET-762+EP by day 100 following initiation of treatment.
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• In Vitro:
  Western blot analysis. Cell line: NUT carcinoma patient cell lines (TC-797 and PER-403). Concentration: 1 μM. Incubation time: 6 h. Result: Results in greater loss of MYC protein.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

EP31670

Quick Database Links

Gene Symbol

Epigenetic Reader Domain