ABBV-744

SKU: orb1225666

Description

ABBV-744 (ABBV744) is a potent, BDII-selective BET bromodomain inhibitor, ABBV-744 is a potent, selective inhibitor of the AR transcription activity; induces tumor growth inhibition in LNCaP and MDA-Pca-2b xenograft models.Prostate Cancer Phase 1 Clinical.

Key Properties

• CAS Number: 2138861-99-9
• MW: 491.563
• Purity: >98% (HPLC)
• Formula: C₂₈H₃₀FN₃O₄
• SMILES: O=C(C(N1)=CC(C(C2=CC(C(C)(O)C)=CC=C2OC3=C(C)C=C(F)C=C3C)=CN4C)=C1C4=O)NCC
• Target: Bromodomain
• Solubility: DMSO: 10 mM （ < 1 mg/ml refers to the product slightly soluble or insoluble )

Bioactivity

• In Vivo:
  Animal model: Mice. Dosage: 4.7 mg/kg (Pharmacokinetic Analysis). Administration: Oral gavage; 28 days. Result: Caused a delay in tumor growth and displayed equivalent or better antitumor activity compared with ABBV-075. Animal model: Sprague-Dawley rats. Dosage: 30 mg/kg (Pharmacokinetic Analysis). Administration: 14 days. Result: Produced significant antitumor activity.
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• In Vitro:
  Western blot analysis. Cell line: LNCaP cells. Concentration: 90 nM. Incubation time: 0~24 hours. Result: Downregulated the expression of KLK2 and MYC genes. Cell Cycle Analysis Cell line: LNCaP cells. Concentration: 90 nM. Incubation time: 0~72 hours. Result: Induced cell cycle arrest in G1 followed by senescence.
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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

ABBV744

Quick Database Links

Gene Symbol

Bromodomain