CWP232228, a highly potent selective Wnt/β-catenin signaling inhibitor, antagonizes binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 suppresses tumor formation and metastasis without toxicity through the inhibition of the growth of breast and liver cancer stem cells (CSCs).
IC50&Target
Wnt/β-catenin
体外研究
CWP232228 (0.01-100 μM; 48 hours) inhibits cell proliferation with IC50 values are 2 and 0.8 μM in mouse (4T1) and human (MDA-MB-435) breast cancer cell lines, respectively.
CWP232228 (0.01-10 μM; 48 hours) inhibits cell proliferation with IC50s of 2.566, 2.630, and 2.596 μM in Hep3B, Huh7 and HepG2 cells, respectively.
Cell Proliferation Assay
Cell Line:
Mouse (4T1) and human (MDA-MB-435) breast cancer cell lines
Concentration:
0.01, 0.1, 1, 10, 100 μM
Incubation Time:
48 hours
Result:
IC50s were 2 and 0.8 μM for 4T1 and MDA-MB-435 cell lines, respectively.
Cell Proliferation Assay
Cell Line:
Hepatocellular carcinoma cell lines HepG2, Huh7, and Hep3B
Concentration:
0.01, 0.1, 0.5, 1, 5, 10 μM
Incubation Time:
48 hours
Result:
IC50s were 2.566, 2.630, and 2.596 μM for Hep3B, Huh7 and HepG2 cells, respectively.
体内研究
CWP232228 (100 mg/kg, administered i.p.; daily; 21days for mice bearing 4T1 cell tumors; 60 days for mice bearing MDA-MB-435 cell tumors) results in a significant reduction in tumor volume.
Animal Model:
7-week-old female Balb/c and NOD/SCID mice bearing 4T1 or MDA-MB-435 cell tumors
Dosage:
100 mg/kg
Administration:
Administered i.p.; daily; 21days for mice bearing 4T1 cell tumors, 60 days for mice bearing MDA-MB-435 cell tumors
Result:
Treatment resulted in a significant reduction in tumor volume.
分子式
C33H34N7Na2O7P
分子量
717.62
CAS号
1144044-02-9
运输条件
Room temperature in continental US; may vary elsewhere.