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1mg |
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Other Sizes |
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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].
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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].
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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]. Waldhauer I, et al. Simlukafusp alfa (FAP-IL2v) immunocytokine is a versatile combination partner for cancer immunotherapy. MAbs. 2021 Jan-Dec;13(1):1913791.
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CAS # |
1776942-10-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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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.