Mivebresib

SKU: orb1303860

Description

Mivebresib (ABBV-075) is a potent and selective BET bromodomain inhibitor that displaces BET proteins from acetylated chromatin, suppressing oncogenic transcription factors like MYC and TMPRSS2-ETS fusions. It demonstrates robust antitumor activity in preclinical models of hematologic malignancies and solid tumors, supporting its investigation in cancer research.

Research Area

Cell Biology, Epigenetics & Chromatin

Key Properties

• CAS Number: 1445993-26-9
• MW: 459.47
• Purity: 99.32%
• Formula: C₂₂H₁₉F₂N₃O₄S
• SMILES: O(C1=C(C=2C3=C(C(=O)N(C)C2)NC=C3)C=C(NS(CC)(=O)=O)C=C1)C4=C(F)C=C(F)C=C4
• Target: Apoptosis,Epigenetic Reader Domain
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.18 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:< 1 mg/mL (insoluble or slightly soluble);DMSO:250 mg/mL (544.11 mM)

Bioactivity

• Target IC50:
  BET:1.5 nM(ki)
• In Vivo:
  ABBV-075 has comparable or superior efficacies to standard of care agents in flank xenograft mouse models of non-small-cell and small cell lung cancers, pancreatic, breast, prostate, head & neck cancers, multiple myeloma, diffuse large B cell lymphoma and leukemia.
• In Vitro:
  Mivebresib exhibits robust single agent activity in cell viability assays across cancer cell lines derived from solid tumors, leukemia and lymphomas. It could disrupt cell cycle control leading to G1 arrest followed by senescence, inhibit oncogenesis drivers leading to apoptosis, and potentially target tumor microenvironment to provide additional therapeutic benefit.

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

Inhibitor, EpigeneticReaderDomain, Epigenetic Reader Domain, inhibit, Mivebresib, ABBV 075, ABBV-075, ABBV075, Apoptosis, BET

Compound Identifiers

PubChem CID

71600087