IITZ-01

SKU: orb1225887

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.

Key Properties

• CAS Number: 1807988-47-1
• MW: 482.523
• Purity: >98% (HPLC)
• Formula: C₂₆H₂₃FN₈O
• SMILES: FC1=CC=C(NC2=NC(N3CCOCC3)=NC(NC4=CC=C(C5=NC6=CC=CC=C6N5)C=C4)=N2)C=C1
• Target: Autophagy
• Solubility: DMSO : 150 mg/mL 310.87 mM; H2O : < 0.1 mg/mL

Bioactivity

• 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.
• 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.

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

Autophagy inhibitor IITZ-01

Quick Database Links

Gene Symbol

Autophagy