WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 407993
CAS#: 1807988-47-1
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
Name: IITZ-01
CAS#: 1807988-47-1
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
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >3 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 482.5234 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
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.
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
