| Identification | Back Directory | [Name]
IZCZ-3 | [CAS]
2223019-53-0 | [Synonyms]
IZCZ-3
9H-Carbazole, 9-ethyl-3-[1-(4-methoxyphenyl)-4,5-bis[4-(4-methyl-1-piperazinyl)phenyl]-1H-imidazol-2-yl]- | [Molecular Formula]
C46H49N7O | [MDL Number]
MFCD31813634 | [MOL File]
2223019-53-0.mol | [Molecular Weight]
715.93 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 5 mg/mL (6.98 mM; ultrasonic and warming and heat to 80°C) | [form ]
Solid | [color ]
Off-white to pink |
| Hazard Information | Back Directory | [Uses]
IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity[1]. | [Biological Activity]
IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity[1].
IZCZ-3 (2.1 μM-15.9 μM; 24 hours) significantly inhibits SiHa, HeLa, Huh7, and A375 cancer cell proliferation (IC50s of 3.3, 2.1，4.1, and 4.2 μM, respectively). IZCZ-3 induces only weak growth inhibition in the BJ fibroblasts (IC50=15.9 μM) and mouse mesangial cells (IC50=15.6 μM), suggesting that IZCZ-3 is more effective against cancer cells than against c-MYC-independent normal cells[1]. IZCZ-3 (0-5 μM; 12 hours) induces an apparent accumulation of cells in the G0/G1 phase in SiHa cells in a dose-dependent manner[1].
IZCZ-3 (20, 10, and 5 mg/kg; intraperitoneally; every other day for 24 days) inhibits tumor growth in BALB/c nude mice with SiHa human cervical squamous cancer xenograft[1]. | [in vivo]
IZCZ-3 (20, 10, and 5 mg/kg; intraperitoneally; every other day for 24 days) inhibits tumor growth in BALB/c nude mice with SiHa human cervical squamous cancer xenograft[1]. | Animal Model: | BALB/c nude mice (5 weeks old) bearing SiHa human cervical squamous cancer xenograft model[1] | | Dosage: | 20, 10, and 5 mg/kg | | Administration: | Treated intraperitoneally; every other day for 24 days | | Result: | Treatment with 20, 10, and 5 mg/kg resulted in a significant reduction in tumor weight with tumor growth inhibition (TGI) of 69%, 64%, and 57%, respectively. Displayed time-dependent inhibition of tumor growth. |
| [References]
[1]. Hu MH, et al. Discovery of a New Four-Leaf Clover-Like Ligand as a Potent c-MYC Transcription Inhibitor Specifically Targeting the Promoter G-Quadruplex. J Med Chem. 2018 Mar 22;61(6):2447-2459. |
|
|