CWP232228

SKU: orb1940802

Description

CWP232228, a potent and selective Wnt / β-catenin signaling inhibitor, antagonizes the binding of β-catenin to T-cell factor (TCF) in the nucleus. CWP232228 inhibits the formation and metastasis of tumors by inhibiting the growth of breast cancer and liver cancer stem cells (CSC) without toxicity.(In Vitro):CWP232228 (0.01-100 μM; 48 hours) inhibited cell proliferation, and IC50 values in mouse (4T1) and human (MDA-MB-435) breast cancer cell lines were 2 and 0.8 μM, respectively. CWP232228 (0.01-10 μM; 48 hours) inhibited cell proliferation in Hep3B, Huh7 and HepG2 cells with IC50 of 2.566, 2.630 and 2.596 μM, respectively.(In Vivo):CWP232228 (100 mg/kg, administered i.p.; daily; mice with 4T1 cell tumors for 21 days; mice with MDA-MB-435 cell tumors for 60 days) resulted in a significant reduction in tumor volume.

Key Properties

• CAS Number: 1144044-02-9
• MW: 717.63
• Purity: >98% (HPLC)
• Formula: C₃₃H₃₄N₇Na₂O₇P
• SMILES: Cn1cc2cccc(CN3C[C@@H]4N(N(CC=C)CC(=O)N4[C@@H](Cc4ccc(OP(=O)(O[Na])O[Na])cc4)C3=O)C(=O)NCc3ccccc3)c2n1
• Target: Wnt/beta/catenin
• Solubility: In Vitro: H2O : 62.5 mg/mL (87.09 mM)

Bioactivity

• In Vivo:
  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.
• In Vitro:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

Wnt/beta/catenin