| Identification | Back Directory | [Name]
IITZ-01 | [CAS]
1807988-47-1 | [Synonyms]
IITZ-01
CS-2857
Autophagy inhibitor IITZ-01
AUTOPHAGY INHIBITOR;IITZ 01;IITZ01
AUTOPHAGY INHIBITOR IITZ-01;IITZ 01;IITZ01
N-[4-(1H-Benzimidazol-2-yl)phenyl]-N'-(4-fluorophenyl)-6-(4-morpholinyl)-1,3,5-triazine-2,4-diamine
1,3,5-Triazine-2,4-diamine, N2-[4-(1H-benzimidazol-2-yl)phenyl]-N4-(4-fluorophenyl)-6-(4-morpholinyl)- | [Molecular Formula]
C26H23FN8O | [MDL Number]
MFCD31746904 | [MOL File]
1807988-47-1.mol | [Molecular Weight]
482.51 |
| Chemical Properties | Back Directory | [Boiling point ]
747.0±70.0 °C(Predicted) | [density ]
1.420±0.06 g/cm3(Predicted) | [storage temp. ]
Keep in dark place,Inert atmosphere,2-8°C | [solubility ]
DMSO:100.0(Max Conc. mg/mL);207.24(Max Conc. mM) | [form ]
Solid | [pka]
11.55±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
IITZ-01 is a potent lysosomotropic autophagy inhibitor with single-agent antitumor activity, with an IC50 of 2.62 μM for PI3Kγ. | [Biological Activity]
IITZ-01 is a potent lysosomal autophagy inhibitor with antitumor activity, with IC50 value of 2.62 μM for PI3Kγ. | [in vivo]
IITZ-01 (45 mg/kg, ip 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- Foxn nu 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. | | [target]
| PI3Kγ 2.62 μM (IC 50 ) | Autophagy < /span> | | [IC 50]
PI3Kγ: 2.62 μM (IC50); Autophagy | [storage]
Store at -20°C | [References]
[1] Guntuku L, et al. IITZ-01, a novel potent lysosomotropic autophagy inhibitor, has single-agent antitumor efficacy in triple-negative breast cancer in vitro and in vivo. Oncogene. 2018 Aug 30. DOI:10.1038/s41388-018-0446-2 |
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