| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
FGFR3
Recifercept targets fibroblast growth factors (FGFs) that would otherwise bind to mutant FGFR3. In achondroplasia, activating mutations in FGFR3 lead to constitutive signaling that inhibits bone growth. Recifercept acts as a soluble receptor that sequesters FGF ligands, preventing them from binding to the mutant FGFR3 on the cell surface. This reduces the negative signaling and allows for normal skeletal development. |
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| ln Vitro |
In vitro, Recifercept has been shown to bind to FGF ligands, acting as a decoy to reduce the amount of FGFs available to bind to mutant FGFR3 receptors. Its activity is typically assessed using binding assays that measure its affinity for various FGFs. These studies confirm its mechanism of action as a ligand trap for FGFR3.
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| ln Vivo |
In vivo, Recifercept has been studied in animal models and clinical trials for achondroplasia. By acting as a decoy receptor, it is expected to restore normal bone growth in patients with achondroplasia. Its efficacy is evaluated by measuring bone growth and other skeletal parameters in preclinical models and clinical studies.
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| Enzyme Assay |
Cell-free assays for Recifercept typically involve measuring its binding affinity to FGF ligands using surface plasmon resonance (SPR) or enzyme-linked immunosorbent assay (ELISA). These assays are used to characterize the decoy protein's potency and specificity for various FGFs. The purity and integrity of the recombinant protein are assessed using SDS-PAGE and size-exclusion chromatography.
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| Cell Assay |
In vitro cellular assays are conducted to evaluate the functional activity of Recifercept. Cells expressing mutant FGFR3 are treated with FGFs in the presence or absence of the decoy protein. FGFR3 phosphorylation and downstream signaling are measured to assess the inhibition of mutant FGFR3 activity. These assays confirm that Recifercept effectively sequesters FGF ligands and blocks mutant FGFR3 signaling.
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| Animal Protocol |
In vivo animal experiments typically involve models of achondroplasia. Animals are administered Recifercept. Bone growth and other skeletal parameters are measured to assess the compound's efficacy in restoring normal bone development. These studies are crucial for demonstrating the in vivo activity of the decoy protein.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of Recifercept are characteristic of a recombinant soluble receptor protein. It is designed to have a favorable half-life to support therapeutic dosing. When administered systemically, it achieves sufficient exposure to act as a ligand trap for FGFs. Its pharmacokinetic profile supports its use in the treatment of achondroplasia.
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| Toxicity/Toxicokinetics |
The toxicity profile of Recifercept is not extensively documented but is likely to be favorable for a recombinant protein. As a decoy receptor, it is expected to have a targeted mechanism of action with limited off-target effects. Preclinical studies would typically involve acute and chronic dosing in animal models to assess safety margins and identify potential toxicities.
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| References | |
| Additional Infomation |
Recifercept is a recombinant human soluble FGFR3 being developed as a treatment for achondroplasia. It functions as a decoy receptor to sequester FGF ligands and prevent the activation of mutant FGFR3. By doing so, it restores normal bone growth. The compound is currently in clinical development.
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| CAS # |
2226238-09-9
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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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