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IITZ-01
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
IITZ-01图片
CAS NO:1807988-47-1
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW) 482.52
Formula C26H23FN8O
CAS No. 1807988-47-1
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO:>10mM
Water: N/A
Ethanol: N/A
Chemical Name N2-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-N4-(4-fluorophenyl)-6-morpholino-1,3,5-triazine-2,4-diamine
Synonyms IITZ 01; IITZ-01; IITZ01
实验参考方法
In Vitro

In vitro activity: IITZ-01 is a novel and potent lysosomotropic autophagy inhibitor which has single-agent antitumor efficacy in triple-negative breast cancer in vitro and in vivo. Treatment with IITZ-01 resulted in the vacuolated appearance of cells due to their specific accumulation in lysosomes. In addition, these basic compounds also deacidify lysosomes as evidenced by the decrease in lysotracker red staining and inhibit maturation of lysosomal enzymes leading to lysosomal dysfunction. IITZ-01 and IITZ-02 enhance autophagosome accumulation but inhibit autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy. Interestingly, compound IITZ-01 exhibited more than 10-fold potent autophagy inhibition along with 12- to 20-fold better cytotoxic action than CQ. IITZ-01 and IITZ-02 also abolished mitochondrial membrane potential and triggered apoptosis through the mitochondria-mediated pathway. Furthermore, IITZ-01 and IITZ-02 displayed potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model with IITZ-01exhibiting superior anticancer efficacy. Overall, these data demonstrate that IITZ-01 is potent autophagy inhibitor with single-agent anticancer activity and awaits further preclinical development as potential anticancer therapeutic.


Kinase Assay:


Cell Assay: compound IITZ-01 exhibited more than 10-fold potent autophagy inhibition along with 12- to 20-fold better cytotoxic action than CQ.

In VivoIITZ-01 and IITZ-02 displayed potent antitumor action in vivo through autophagy inhibition and apoptosis induction in MDA-MB-231 breast cancer xenograft model with IITZ-01exhibiting superior anticancer efficacy. Overall, these data demonstrate that IITZ-01 is potent autophagy inhibitor with single-agent anticancer activity and awaits further preclinical development as potential anticancer therapeutic.
Animal model
Formulation & Dosage
References Oncogene. 2018 Aug 30. doi: 10.1038/s41388-018-0446-2.