A1874

SKU: orb1225722

Description

A1874 (A-1874) is a nutlin-based and BRD4-degrading PROTAC with DC50 of 32 nM (induce BRD4 degradation in cells); A1874 is more effective in inhibiting proliferation of many cancer cell lines with wild type p53 than was a corresponding VHL-utilizing PROTAC with similar potency and efficacy to degrade BRD4; demonstrates synergistic antiproliferative effect via simultaneous degradation of BRD4 and stabilization of p53.

Key Properties

• CAS Number: 2064292-12-0
• MW: 1173.597
• Purity: >98% (HPLC)
• Formula: C₅₈H₆₂Cl₃F₂N₉O₇S
• SMILES: O=C([C@@H]1N[C@@H](CC(C)(C)C)[C@](C#N)(C2=CC=C(Cl)C=C2F)[C@H]1C3=CC=CC(Cl)=C3F)NC4=CC=C(C(NCCOCCOCCOCCNC(C[C@H]5C6=NN=C(C)N6C7=C(C(C)=C(C)S7)C(C8=CC=C(Cl)C=C8)=N5)=O)=O)C=C4OC
• Target: PROTAC
• Solubility: DMSO : 150 mg/mL 127.81 mM;H2O : < 0.1 mg/mL

Bioactivity

• In Vitro:
  Western blot analysis. Cell line: HCT116 cells. Concentration: 0-10 μM. Incubation time: 24 hours. Result: Induced a dosedependent knockdown of BRD4 levels, with near-maximum knockdown by 100 nM. Increased p53 levels and showed dose-dependent p53 stabilization.
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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

A-1874

Quick Database Links

Gene Symbol

PROTAC