| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Wnt ligand[1]
Ipafricept targets Wnt ligands by acting as a decoy receptor. The Frizzled-8 extracellular domain portion of the fusion protein binds to Wnt ligands, sequestering them and preventing their interaction with endogenous Frizzled receptors on the cell surface. This blocks the activation of Wnt/β-catenin signaling, a pathway that is frequently dysregulated in cancer and is associated with cancer stem cell maintenance, tumor growth, and metastasis. By inhibiting Wnt signaling, Ipafricept aims to suppress tumor progression. |
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| ln Vitro |
Ipafricept (10 μg/mL) inhibits the pro-proliferative and pro-migratory effects of the peptide RL-QN15 on human embryonic stem cells (hESCs). It reverses RL-QN15-induced activation of the Wnt/β-catenin signaling pathway, thereby counteracting its effects on hESC proliferation, migration, and stemness. These in vitro studies demonstrate the compound's ability to functionally block Wnt signaling and its downstream biological effects. Ipafricept's activity as a Wnt inhibitor has been characterized in various cell-based assays.
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| ln Vivo |
Ipafricept demonstrates significant in vivo antitumor activity in xenograft mouse models. In pancreatic cancer xenograft models, Ipafricept administered intraperitoneally at 10 mg/kg weekly or 25 mg/kg every two weeks for 42 days, in combination with Gemcitabine or Nab-paclitaxel, significantly enhances tumor growth inhibition. In ovarian cancer xenograft models, Ipafricept (45 mg/kg every two weeks, i.p., for 42 days) combined with Nab-paclitaxel shows greater antitumor activity than Carboplatin. In a mouse full-thickness skin wound model, Ipafricept (10 mg/kg, s.c., on days 0 and 3) competes with RL-QN15 for FZD8 binding, reducing RL-QN15-mediated Wnt/β-catenin pathway activation.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for Ipafricept typically involves a binding assay to assess its interaction with Wnt ligands. Recombinant Wnt proteins are incubated with Ipafricept, and the binding affinity is measured using surface plasmon resonance (SPR) or ELISA-based methods. Alternatively, a competition assay can be performed where labeled Wnt ligands are incubated with Ipafricept and the displacement is measured. The ability of Ipafricept to block Wnt ligand binding to Frizzled receptors can also be assessed using cell-free receptor-binding assays.
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| Cell Assay |
The in vitro cellular assay for Ipafricept typically uses cells with active Wnt/β-catenin signaling, such as cancer cell lines or human embryonic stem cells (hESCs). Cells are treated with varying concentrations of Ipafricept, and Wnt/β-catenin pathway activity is measured using a TCF/LEF-luciferase reporter assay. The compound's effects on cell proliferation, migration, and stemness are assessed using standard assays such as cell viability, wound healing, and colony formation assays. In hESCs, the reversal of RL-QN15-induced effects is a key readout.
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| Animal Protocol |
In vivo animal studies for Ipafricept typically involve xenograft tumor models in immunodeficient mice. Mice bearing subcutaneous tumors derived from pancreatic or ovarian cancer cell lines are treated with Ipafricept via intraperitoneal injection at various doses and schedules, alone or in combination with chemotherapeutic agents such as Gemcitabine or Nab-paclitaxel. Tumor growth inhibition is monitored over time. In the full-thickness skin wound model, Ipafricept is administered subcutaneously. Endpoints include tumor volume, Wnt/β-catenin target gene expression, and histological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Ipafricept are not extensively detailed in the available literature. As a fusion protein, its pharmacokinetic properties would be expected to differ from small molecules, with a longer half-life typical of monoclonal antibodies and Fc-fusion proteins. The compound is administered via injection (intraperitoneal or subcutaneous) in animal studies. Specific parameters such as clearance, volume of distribution, and bioavailability have not been reported. Researchers should consult the primary literature for detailed PK information.
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| Toxicity/Toxicokinetics |
Toxicity data for Ipafricept are not extensively reported. As a recombinant fusion protein being investigated for anticancer therapy, toxicological studies would be expected to be conducted as part of preclinical development. However, detailed toxicity data are not available in the public domain. The compound is intended for research use only. Standard safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
Ipafricept (OMP-54F28) is a first-in-class recombinant fusion protein decoy receptor for Wnt ligands, consisting of the Frizzled-8 extracellular domain fused to human IgG1 Fc. It blocks Wnt/β-catenin signaling and has demonstrated anticancer activity in preclinical models of solid tumors, including pancreatic and ovarian cancer. The compound has been investigated in clinical trials for the treatment of solid tumors. However, its clinical development status may have changed, and it has not received regulatory approval. Researchers should consult the latest clinical trial registries for up-to-date information.
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| CAS # |
1391727-24-4
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| Appearance |
Colorless to light yellow liquid
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
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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