IITZ-01

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

IITZ-01（自噬抑制剂 IITZ-01）是一种新型强效溶酶体自噬抑制剂。

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.

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.

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.

Autophagy inhibitor IITZ-01

Autophagy

Autophagy

Autophagy

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1807988-47-1

482.523

C26H23FN8O

>98% (HPLC)

DMSO : 150 mg/mL 310.87 mM; H2O : < 0.1 mg/mL

FC1=CC=C(NC2=NC(N3CCOCC3)=NC(NC4=CC=C(C5=NC6=CC=CC=C6N5)C=C4)=N2)C=C1

N2-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-N4-(4-fluorophenyl)-6-morpholino-1,3,5-triazine-2,4-diamine

(-20℃)

With Ice Pack

≥ 2 years