IZCZ-3 is a potent c-MYC transcription inhibitor with antitumor activity.
体外研究
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.
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.
Cell Proliferation Assay
Cell Line:
SiHa, HeLa, Huh7, and A375 cancer cells (with overexpression of c-MYC protein) and in normal BJ fibroblasts and primary cultured mouse mesangial cells (with relatively low expression of c-MYC protein).
Concentration:
2.1 μM-15.9 μM
Incubation Time:
24 hours
Result:
IC50s of 3.3, 2.1,4.1, and 4.2 μM for SiHa, HeLa, Huh7, and A375 cancer cells; IC50s of 15.9 μM and 15.6 μM for BJ fibroblasts and mouse mesangial cells.
Cell Cycle Analysis
Cell Line:
SiHa cells
Concentration:
0, 1.25, 2.5, and 5 μM
Incubation Time:
12 hours
Result:
Induced an apparent accumulation of cells in the G0/G1 phase (increasing from 61% to 70%) in a dose-dependent manner.
体内研究
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.
Animal Model:
BALB/c nude mice (5 weeks old) bearing SiHa human cervical squamous cancer xenograft model
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.
分子式
C46H49N7O
分子量
715.93
CAS号
2223019-53-0
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
6 months
-20°C
1 month
溶解性数据
In Vitro:
DMSO : 5 mg/mL (6.98 mM; ultrasonic and warming and heat to 80°C)