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MI-3454

CAS No. 2134169-43-8

MI-3454( —— )

Catalog No. M35130 CAS No. 2134169-43-8

MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.

Purity : >98% (HPLC)

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Biological Information

  • Product Name
    MI-3454
  • Note
    Research use only, not for human use.
  • Brief Description
    MI-3454 is an orally active, selective and potent inhibitor of Menin-MLL1 interaction that inhibits the proliferation and induces differentiation of acute leukemia cells with MLL1 translocation or NPM1 mutation.
  • Description
    MI-3454 is an orally active, highly potent and selective menin-MLL1 interaction inhibitor with an IC50 of 0.51 nM. MI-3454 inhibits proliferation, induces differentiation and complete remission or regression of leukemia in mouse models of MLL1-rearranged or NPM1-mutated leukemia through downregulation of key genes involved in leukemogenesis.
  • In Vitro
    Cell Proliferation Assay Cell Line:Murine bone marrow cells transformed with MLL-AF9 or Hoxa9/Meis1 Concentration:0.001, 0.01, 0.1, 1, 10 μM Incubation Time:7 days Result:Demonstrated strong reduction of cell proliferation.RT-PCR Cell Line:Human leukemic cell lines MV-4-11 cells or MOLM13 Concentration:50 nM Incubation Time:6 days Result:Led to downregulated expression of HOXA9 and MEIS1 and expression level of other MLL fusion target genes, including MEF2C, DLX2, HOXA10, PBX3, and FLT3.
  • In Vivo
    Animal Model:8- to 10-week-old female NSG mice (MV-4-11 xenotransplantation model of MLL leukemia) Dosage:120 mg/kg Administration:Orally; one or twice daily for 7 consecutive daysResult:A once-daily treatment was sufficient to block leukemia progression. Animal Model:Female CD-1 mice Dosage:100 mg/kg (PO) or 15 mg/kg (IV) (Pharmacokinetic Analysis) Administration:PO or IV Result:Had a T1/2 of 3.2 hours, a Cmax of 4698 mg/mL for PO. Had a T1/2 of 2.4 hours, a CL of 2375 mL/hours?kg, and a Vss of 5358 mL/kg for IV.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    Histone Methyltransferase
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2134169-43-8
  • Formula Weight
    636.73
  • Molecular Formula
    C32H35F3N8OS
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 31.25 mg/mL (49.08 mM; Ultrasonic )
  • SMILES
    CNc1nc(NC2CCN(Cc3ccc4n(CC56CC(C5)(C6)NC=O)c(cc4c3C)C#N)CC2)c2cc(CC(F)(F)F)sc2n1
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1. Szymon Klossowski, et al. Menin Inhibitor MI-3454 Induces Remission in MLL1-rearranged and NPM1-mutated Models of Leukemia. J Clin Invest. 2020 Feb 3;130(2):981-997.?
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