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Physicochemical Properties
| CAS # | 1776942-10-9 |
| 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) |
Biological Activity
| ln Vitro | Simlukafusp alfa (FAP-IL2v) has binding values of 43±9 pM, 80±20 pM, 660±80 pM, 0.3 nM, and 0.23 nM for huIL-2Rβγ, cyIL-2Rβγ, muIL-2Rβγ, and huFAP, respectively. and 0.5 nM [1]. In vitro, simulukafusp alfa (0-100 nM; 5 days) stimulates NK cells and CD4+/CD8+ T cells, but it does not specifically activate Tregs [1]. In vitro, Cibisatamab- and Cetuximab-mediated T cell-dependent cytotoxicity (TDCC) and antibody-dependent cellular cytotoxicity (ADCC) are both enhanced by Simlukafusp alfa (0-100 nM) [1]. |
| ln Vivo | In mice models of human cancer, simulukafusp alfa (FAP-IL2v) (1 mg/kg; iv; weekly for 4 weeks) works well when combined with processing antibodies[1]. |
| Cell Assay |
Cell Proliferation Assay[1] Cell Types: NK cells, CD4+ and CD8+ T cells Tested Concentrations: 0-100 nM Incubation Duration: 5 days Experimental Results: Induced a dose-dependent proliferation of resting NK cells and resting and activated CD4+ and CD8+ T cells within peripheral blood mononuclear cells (PBMCs). |
| Animal Protocol |
Animal/Disease Models: huCD16-transgenic SCID mice, lung orthotopic xenograft A549 model[1] Doses: 1 mg/kg in combination with 25 mg/kg Cetuximab as single agents Route of Administration: IV, weekly starting at Day 14 for 4 weeks Experimental Results: Achieved greater tumor control than either agent given as monotherapy. decreased tumor volume and tumor growth. Animal/Disease Models: CD-1 mice[1] Doses: 1, 2 or 4 mg/kg Route of Administration: IV (pharmacokinetic/PK Analysis) Experimental Results: pharmacokinetic/PK parameters after first dose of human FAP-IL2v (huFAP-IL2v) in CD-1 mice CD-1 mice (n=10 per group) were given 1, 2, and 4 mg/kg huFAP-IL2v by IV administration once weekly. Multiple IV doses at 1 and 2 mg/kg were administered QW for up to a maximum of three doses, at which point toxicity was observed. Only a single dose was administered to the 4-mg/kg IV treatment group because of toxicity in these treatment groups. Blood was sampled at 0.5, 6, 24, 48, 72, and 168 h. huFAP-IL2v dose (mg/kg) Cmax (μg/mL) AUC0-168h (μg·h/mL per mg/kg) CL (mL/ d |
| References |
[1]. Simlukafusp alfa (FAP-IL2v) immunocytokine is a versatile combination partner for cancer immunotherapy. MAbs. 2021 Jan-Dec;13(1):1913791. |
Solubility Data
| 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 (e.g. IP/IV/IM/SC) Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline) *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). 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)] *Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin → 500 μL Saline) Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO → 100 μLPEG300 → 200 μL castor oil → 650 μL Saline) Injection Formulation 7: Ethanol : Cremophor : Saline = 10： 10 : 80 (i.e. 100 μL Ethanol → 100 μL Cremophor → 800 μL Saline) Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH → 900 μL Corn oil) Injection Formulation 10: EtOH : PEG300：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH → 400 μLPEG300 → 50 μL Tween 80 → 450 μL 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). Oral Formulation 3: Dissolved in PEG400 Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose Oral Formulation 6: Mixing with food powders Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently. (Please use freshly prepared in vivo formulations for optimal results.) |