| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| Other Sizes |
| Targets |
MHC Class II.
|
|---|---|
| ln Vitro |
Eftilagimod alfa (IMP321) is a recombinant fusion protein consisting of the extracellular domain of human LAG-3 fused to an IgG1 Fc region. It binds to MHC class II molecules on APCs with high affinity, leading to APC maturation, increased expression of co-stimulatory molecules (CD80, CD86, CD83), and enhanced cytokine production (IL-12, TNF-alpha). This results in CD8+ T-cell activation, proliferation, and cytotoxicity.
|
| ln Vivo |
Eftilagimod alfa (IMP321) shows anti-tumor activity in preclinical syngeneic mouse models. In tumor-bearing mice, administration of the fusion protein increases CD8+ T-cell infiltration into tumors and reduces tumor growth. It has been evaluated in clinical trials for metastatic melanoma and metastatic breast cancer, demonstrating immune activation and disease stabilization in some patients.
|
| Enzyme Assay |
Not applicable for fusion proteins. Binding affinity of eftilagimod alfa to MHC class II is determined by surface plasmon resonance (SPR). Recombinant human MHC class II (HLA-DR) is immobilized on a sensor chip. Serial dilutions of eftilagimod alfa (0-500 nM) are injected, and KD is calculated (typically low nanomolar range). For cell binding assays, human PBMCs or monocyte-derived dendritic cells are incubated with eftilagimod alfa (0-100 microg/mL) followed by FITC-labeled anti-human IgG secondary antibody, and binding is analyzed by flow cytometry (mean fluorescence intensity).
|
| Cell Assay |
Human PBMCs are isolated from healthy donors. Monocytes are purified and differentiated into immature dendritic cells (iDCs) with GM-CSF and IL-4 for 7 days. iDCs are matured with TNF-alpha (10 ng/mL) for 24 h, then incubated with eftilagimod alfa (0-50 microg/mL) for 24-48 h. DC maturation markers (CD80, CD83, CD86, HLA-DR) are analyzed by flow cytometry. Autologous CD3+ T cells are co-cultured with eftilagimod alfa-treated DCs for 5 days. T-cell proliferation is measured by CFSE dilution or [3H]thymidine incorporation. Cytokine production (IFN-gamma, IL-2, IL-12) in supernatants is measured by ELISA. CD8+ T-cell cytotoxicity against target tumor cells (e.g., MCF-7 breast cancer cells) is assessed by LDH release assay.
|
| Animal Protocol |
No published animal protocol is available for eftilagimod alfa. Generic protocol for LAG-3Ig fusion protein: female C57BL/6 mice (6-8 weeks) are implanted subcutaneously with B16-F10 melanoma cells (5×10⁵) or 4T1 breast cancer cells. When tumors reach ~50-100 mm3, mice are randomized (n=8-10/group). Eftilagimod alfa is administered subcutaneously or intraperitoneally at 1-10 mg/kg twice weekly for 2-3 weeks. Tumor volumes are measured by calipers. At termination, tumors are collected for flow cytometry (CD3+, CD4+, CD8+, FoxP3+, Granzyme B) and immunohistochemistry (CD8, MHC class II). Serum cytokines are measured by multiplex assay. Splenocytes are re-stimulated with tumor antigens for ex vivo IFN-gamma ELISPOT.
|
| ADME/Pharmacokinetics |
As a recombinant fusion protein (LAG-3 with IgG1 Fc, MW ~150 kDa), eftilagimod alfa exhibits antibody-like PK. In humans, subcutaneous administration (1-30 mg) yields Cmax at 24-48 h (Tmax), with a terminal half-life of approximately 7-12 days. Bioavailability is moderate (40-60%). Clearance is low (0.2-0.5 L/day). The Fc region may contribute to prolonged circulation through FcRn-mediated recycling. In preclinical studies, weekly dosing maintains steady-state concentrations.
|
| Toxicity/Toxicokinetics |
No published toxicity data for eftilagimod alfa is available. In clinical trials (Phase I/II), eftilagimod alfa has been well tolerated at doses up to 30 mg subcutaneously every 2 weeks. Most common adverse events are injection site reactions (mild to moderate erythema, swelling, pruritus), fatigue, mild flu-like symptoms (fever, chills, myalgia), and transient lymphopenia. No dose-limiting toxicity or significant immune-related adverse events (pneumonitis, colitis, hepatitis) have been reported, consistent with its APC-activating mechanism distinct from checkpoint inhibitors.
|
| References | |
| Additional Infomation |
Eftilagimod alfa (IMP321) is an investigational immunotherapeutic agent developed by Immutep. It has completed Phase I and Phase II clinical trials in metastatic melanoma (NCT02676869) and metastatic breast cancer (NCT02614833). As of current literature, it has not received regulatory approval. Unlike checkpoint inhibitors that block inhibitory receptors, eftilagimod alfa works by activating APCs, leading to enhanced CD8+ T-cell priming and expansion. It is being evaluated in combination with PD-1 inhibitors (e.g., pembrolizumab) and chemotherapies.
|
| CAS # |
1800476-36-1
|
|---|---|
| Appearance |
Colorless to light yellow liquid
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
