MI-3454

SKU: orb1691204

Description

MI-3454 is a potent, selective, and orally bioavailable Menin-MLL1 interaction inhibitor. It demonstrates anti-proliferative and differentiation-inducing activity in vitro against acute leukemia cells harboring MLL1 rearrangements or NPM1 mutations. In vivo studies in murine leukemia models show it can induce remission by downregulating key leukemogenic genes.

Research Area

Epigenetics & Chromatin

Key Properties

• CAS Number: 2134169-43-8
• MW: 636.73
• Purity: 99.68% (May vary between batches)
• Formula: C₃₂H₃₅F₃N₈OS
• SMILES: CNc1nc(NC2CCN(Cc3ccc4n(CC56CC(C5)(C6)NC=O)c(cc4c3C)C#N)CC2)c2cc(CC(F)(F)F)sc2n1
• Target: Epigenetic Reader Domain,Histone Methyltransferase
• Solubility: DMSO:20 mg/mL (31.41 mM)

Bioactivity

• Target IC50:
  Menin-MLL1:0.51 nM
• In Vivo:
  In 8- to 10-week-old female NSG mice (MV-4-11 xenotransplantation model of MLL leukemia), MI-3454 (120 mg/kg; orally; once or twice daily for 7 consecutive days) is sufficient to block leukemia progression.
• In Vitro:
  In murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1, MI-3454 (0.001, 0.01, 0.1, 1, 10 μM; 7 days) demonstrated a significant reduction in cell proliferation.

Storage & Handling

• Storage: store at low temperature,store under nitrogen | 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

MI 3454, MI3454, MI-3454, HistoneMethyltransferase, Histone Methyltransferase, Menin-MLL

Compound Identifiers

PubChem CID

130443890