| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg | |||
| Other Sizes |
Purity: ≥98%
| Targets |
CWP232228 targets the Wnt/β-catenin signaling pathway by antagonizing the binding of β-catenin to T-cell factor (TCF) in the nucleus. By blocking this protein-protein interaction, it prevents the transcription of Wnt target genes involved in cell proliferation, survival, and stem cell self-renewal. This mechanism is distinct from upstream inhibition of Wnt ligand production or receptor activation.
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| ln Vitro |
CWP232228 (0.01-100 μM; 48 hours) suppresses cell growth with IC50 values of 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) suppresses cell growth in Hep3B, Huh7, and HepG2 cells with IC50 of 2.566, 2.630, and 2.596 μM, respectively [2].
In vitro, CWP232228 exhibits potent anti-proliferative activity against various cancer cell lines. It inhibits proliferation in breast cancer cells with IC50 values of 2 µM (4T1, mouse) and 0.8 µM (MDA-MB-435, human), as well as in hepatocellular carcinoma cells (Hep3B, Huh7, HepG2; IC50 ~2.6 µM). This activity is attributed to its ability to suppress the growth of cancer stem cells (CSCs). |
| ln Vivo |
Tumor volume was significantly reduced by CWP232228 (100 mg/kg, i.p.; daily; 21 days for mice with 4T1 cell tumors; 60 days for mice with MDA-MB-435 cell tumors) [1].
In vivo, CWP232228 demonstrates significant antitumor efficacy in animal models. Daily intraperitoneal dosing at 100 mg/kg significantly reduces tumor burden in breast and liver cancer models. The compound suppresses tumor formation and metastasis without significant toxicity. These findings support its potential as a novel therapeutic agent for Wnt-driven cancers. |
| Enzyme Assay |
In cell-free binding assays, CWP232228's activity is evaluated by measuring its ability to disrupt the interaction between β-catenin and TCF. The assay typically involves incubating purified β-catenin protein with a TCF-derived peptide or DNA-binding domain in the presence of varying concentrations of the compound. The extent of the protein-protein interaction is measured using techniques such as fluorescence polarization, surface plasmon resonance, or ELISA, and the IC50 is calculated.
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| Cell Assay |
Cell proliferation assay[1]
Cell Types: mouse (4T1) and human (MDA-MB-435) Breast cancer cell lines Tested Concentrations: 0.01, 0.1, 1, 10, 100 μM Incubation Duration: 48 hrs (hours) Experimental Results: IC50 is 2 respectively and 0.8 μM for 4T1 and MDA-MB-435 cell lines respectively. Cell proliferation assay [2] Cell Types: Hepatoma cell lines HepG2, Huh7 and Hep3B Tested Concentrations: 0.01, 0.1, 0.5, 1, 5, 10 μM Incubation Duration: 48 hrs (hours) Experimental Results: IC50 are 2.566, 2.630 and 2.596 μM respectively for Hep3B , Huh7 and HepG2 cells. In vitro cell-based experiments with CWP232228 typically involve culturing cancer cell lines, such as breast cancer (4T1, MDA-MB-435) or hepatocellular carcinoma (Hep3B, Huh7, HepG2) cells. Cells are treated with various concentrations of the compound for 48-72 hours, and cell viability is assessed using standard assays such as MTT or CellTiter-Glo. The effect on Wnt/β-catenin signaling is confirmed by measuring the expression of Wnt target genes (e.g., AXIN2, MYC) using qPCR. |
| Animal Protocol |
Animal/Disease Models: 7weeks old female Balb/c and NOD/SCID (severe combined immunodeficient) mouse harboring 4T1 or MDA-MB-435 cell tumors [1]
Doses: 100 mg/kg Route of Administration: intraperitoneal (ip) injection; daily; for 4T1 cell-bearing tumors It was 21 days for mice with tumors and 60 days for mice with MDA-MB-435 cell tumors. Experimental Results: Treatment resulted in a significant reduction in tumor volume. In vivo animal experiments with CWP232228 typically involve xenograft models in immunodeficient mice. Mice are inoculated with cancer cells (e.g., breast or liver cancer cells) to establish tumors. When tumors reach a certain size, animals are treated with CWP232228 via intraperitoneal injection at a dose of 100 mg/kg daily. Tumor volumes are measured periodically, and at the end of the study, tumors are excised for analysis of Wnt signaling markers. |
| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CWP232228 sodium. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. It is administered via intraperitoneal injection in in vivo studies. Its bioavailability, half-life, and tissue distribution have not been well established in the available literature.
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| Toxicity/Toxicokinetics |
In preclinical studies, CWP232228 has been reported to suppress tumor formation and metastasis without significant toxicity. No specific toxicological data is publicly available beyond these general observations. The compound is for research use only and is not intended for human therapeutic applications. Further studies would be needed to fully characterize its safety profile.
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| References |
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| Additional Infomation |
CWP232228 sodium is a potent and selective inhibitor of Wnt/β-catenin signaling with a molecular formula of C33H34N7Na2O7P and a molecular weight of 717.62. It is also known as disodium [4-[[(6S,9aS)-1-(benzylcarbamoyl)-8-[(2-methylindazol-7-yl)methyl]-4,7-dioxo-2-prop-2-enyl-3,6,9,9a-tetrahydropyrazino[2,1-c][1,2,4]triazin-6-yl]methyl]phenyl] phosphate. It is a valuable research tool for studying the Wnt/β-catenin pathway and cancer stem cell biology. It is not approved for clinical use.
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| Molecular Formula |
C33H34N7NA2O7P
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| Molecular Weight |
717.619069576263
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| Exact Mass |
717.205
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| CAS # |
1144044-02-9
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| Related CAS # |
1144044-02-9 (sodium);1144045-59-9 (free acid);
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| PubChem CID |
71509158
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
50
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| Complexity |
1210
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| Defined Atom Stereocenter Count |
2
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| SMILES |
P(=O)([O-])([O-])OC1C=CC(=CC=1)C[C@H]1C(N(CC2=CC=CC3=CN(C)N=C23)C[C@@H]2N(C(NCC3C=CC=CC=3)=O)N(CC=C)CC(N21)=O)=O.[Na+].[Na+]
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| InChi Key |
KKMKZLQVDAGSOA-GDUXWEAWSA-L
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| InChi Code |
InChI=1S/C33H36N7O7P.2Na/c1-3-16-38-22-30(41)39-28(17-23-12-14-27(15-13-23)47-48(44,45)46)32(42)37(20-26-11-7-10-25-19-36(2)35-31(25)26)21-29(39)40(38)33(43)34-18-24-8-5-4-6-9-24/h3-15,19,28-29H,1,16-18,20-22H2,2H3,(H,34,43)(H2,44,45,46)/q2*+1/p-2/t28-,29-/m0../s1
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| Chemical Name |
Sodium
4-(((6S,9aS)-2-Allyl-1-(benzylcarbamoyl)-8-((2-methyl-2H-indazol-7-yl)methyl)-4,7-dioxooctahydro-2H-pyrazino[2,1-c][1,2,4]triazin-6-yl)methyl)phenyl
phosphate
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| Synonyms |
CWP232228 CWP-232228 CWP 232228 CWP232228 sodium,
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O : ~62.5 mg/mL (~87.09 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (69.67 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3935 mL | 6.9675 mL | 13.9350 mL | |
| 5 mM | 0.2787 mL | 1.3935 mL | 2.7870 mL | |
| 10 mM | 0.1393 mL | 0.6967 mL | 1.3935 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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