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IITZ-01

CAS No. 1807988-47-1

IITZ-01( Autophagy inhibitor IITZ-01 )

Catalog No. M12762 CAS No. 1807988-47-1

IITZ-01 (Autophagy inhibitor IITZ-01) is a novel potent lysosomotropic autophagy inhibitor.

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    IITZ-01
  • Note
    Research use only, not for human use.
  • Brief Description
    IITZ-01 (Autophagy inhibitor IITZ-01) is a novel potent lysosomotropic autophagy inhibitor.
  • Description
    IITZ-01 (Autophagy inhibitor IITZ-01) is a novel potent lysosomotropic autophagy inhibitor, exhibits >10-fold potent autophagy inhibition along with 12- to 20-fold better cytotoxic action than Chloroquine; enhances autophagosome accumulation but inhibit autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy, also abolishes mitochondrial membrane potential and triggers apoptosis through the mitochondria-mediated pathway (TNBC cells IC50=1.54 uM, 48 h); displays potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model.
  • In Vitro
    IITZ-01 (0-2 μM, 24 h) enhances autophagosomes formation as indicated by increased expression of LC3-II levels time- and dose-dependently intriple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453). IITZ-01 also demonstrates potent autophagy inhibitory activity in other breast, lung, and colon cancer cells.Western Blot Analysis Cell Line:Triple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453).Concentration:0-2 μM.Incubation Time:24 hours.Result:Enhanced autophagosomes formation as indicated by increased expression of LC3-II levels.
  • In Vivo
    IITZ-01 (45 mg/kg, i.p. every alternate day for 4 weeks) inhibits average breast tumor growth when compared with control from third day of treatment in triple-negative breast tumor models in mice. Animal Model:MDA-MB-231 (TNBC)/green fluorescent protein (GFP) orthotropic breast cancer xenografts were developed in CrTac:NCr-Foxnnu BALB/c female nude mice.Dosage:45 mg/kg.Administration:Intraperitoneal every alternate day for 4 weeks.Result:Inhibited average breast tumor growth when compared with control from third day of treatment.
  • Synonyms
    Autophagy inhibitor IITZ-01
  • Pathway
    Autophagy
  • Target
    Autophagy
  • Recptor
    Autophagy
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    1807988-47-1
  • Formula Weight
    482.523
  • Molecular Formula
    C26H23FN8O
  • Purity
    >98% (HPLC)
  • Solubility
    DMSO : 150 mg/mL 310.87 mM; H2O : < 0.1 mg/mL
  • SMILES
    FC1=CC=C(NC2=NC(N3CCOCC3)=NC(NC4=CC=C(C5=NC6=CC=CC=C6N5)C=C4)=N2)C=C1
  • Chemical Name
    N2-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-N4-(4-fluorophenyl)-6-morpholino-1,3,5-triazine-2,4-diamine

Shipping & Storage Information

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

Reference

1. Guntuku L, et al. Oncogene. 2018 Aug 30. doi: 10.1038/s41388-018-0446-2.
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