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MedKoo CAT#: 407993
Description: IITZ-01 (Autophagy inhibitor IITZ-01) is a novel potent lysosomotropic autophagy inhibitor. IITZ-01 enhances autophagosome accumulation but inhibit autophagosomal degradation by impairing lysosomal function, finally resulting in the inhibition of autophagy. IITZ-01 exhibited more than 10-fold potent autophagy inhibition along with 12- to 20-fold better cytotoxic action than CQ. IITZ-01 is potent autophagy inhibitor with single-agent anticancer activity and awaits further preclinical development as potential anticancer therapeutic.
MedKoo Cat#: 407993
Chemical Formula: C26H23FN8O
Exact Mass: 482.1979
Molecular Weight: 482.5234
Elemental Analysis: C, 64.72; H, 4.80; F, 3.94; N, 23.22; O, 3.32
Synonym: IITZ-01; IITZ 01; IITZ01; Autophagy inhibitor IITZ-01;
IUPAC/Chemical Name: N2-(4-(1H-benzo[d]imidazol-2-yl)phenyl)-N4-(4-fluorophenyl)-6-morpholino-1,3,5-triazine-2,4-diamine
InChi Key: XGEDDGLPNSLBFE-UHFFFAOYSA-N
InChi Code: InChI=1S/C26H23FN8O/c27-18-7-11-20(12-8-18)29-25-32-24(33-26(34-25)35-13-15-36-16-14-35)28-19-9-5-17(6-10-19)23-30-21-3-1-2-4-22(21)31-23/h1-12H,13-16H2,(H,30,31)(H2,28,29,32,33,34)
SMILES Code: FC1=CC=C(NC2=NC(N3CCOCC3)=NC(NC4=CC=C(C5=NC6=CC=CC=C6N5)C=C4)=N2)C=C1
Autophagy is a homeostatic process that recycles damaged organelles and long-lived proteins by delivering them in double-membrane vesicles to lysosomes for degradation. Autophagy has a prominent role in survival, proliferation, and resistance of tumors in metabolic and chemotherapeutic stress conditions. Clinical trials with chloroquine-a known autophagy inhibitor-were unable to achieve complete autophagy inhibition in vivo, warranting the search for more potent autophagy inhibitors
1: Guntuku L, Gangasani JK, Thummuri D, Borkar RM, Manavathi B, Ragampeta S,
Vaidya JR, Sistla R, Vegi NGM. IITZ-01, a novel potent lysosomotropic autophagy
inhibitor, has single-agent antitumor efficacy in triple-negative breast cancer
in vitro and in vivo. Oncogene. 2019 Jan;38(4):581-595. doi:
10.1038/s41388-018-0446-2. Epub 2018 Aug 30. PubMed PMID: 30166591.