CWP232228

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)[1].

Research Areas >> Cancer

Signaling Pathways >> Stem Cell/Wnt >> Wnt

Wnt/β-catenin[1]

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[1]. 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[2]. Cell Proliferation Assay[1] 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[2] 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.

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[1]. Animal Model: 7-week-old female Balb/c and NOD/SCID mice bearing 4T1 or MDA-MB-435 cell tumors[1] 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.

[1]. Jang GB, et al. Wnt/β-Catenin Small-Molecule Inhibitor CWP232228 Preferentially Inhibits the Growth of Breast Cancer Stem-like Cells. Cancer Res. 2015 Apr 15;75(8):1691-702.

[2]. Kim JY, et al. Oncotarget. 2016 Apr 12;7(15):20395-409. CWP232228 targets liver cancer stem cells through Wnt/β-catenin signaling: a novel therapeutic approach for liver cancer treatment.