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Physicochemical Properties
| CAS # | 2055491-00-2 |
| Appearance | Typically exists as solid at room temperature |
| 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
| Targets | IL-3 |
| ln Vitro | Tagraxofusp (0-1367 pM; 72 h) suppresses the proliferation of MM cells produced by pDCs and the viability of pDCs. Tagraxofusp (0-136.7 pM; 2-3 weeks) stabilizes osteoblast formation while blocking the generation of osteoclasts and bone resorption [1]. Tagraxofusp (0-13.67 nM; 48 h) acts on stem-like cells in MM that initiate tumors[1]. |
| ln Vivo | In a subcutaneous INA-6 MM xenograft model, tagraxofusp (12-50 μg/kg; iv; five times per week for three weeks) prolongs the longevity of SCID-hu mice and inhibits the formation of tumors generated by pDC[1]. In CB-17 mice in a subcutaneous MM xenograft model, Tagraxofusp (16 μg/kg; iv; five times per week for one week) increases the anti-MM activity of 2.5 mg/kg Pomalidomide[1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: Cancer stem-like cells in MM Tested Concentrations: 0 nM, 0.013 nM, 0.13 nM, 1.3 nM, 13.67 nM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibits cancer stem-like cells with s of 30 pM (pDCs), 50 nM (MM-SP-Oct4 cells), 75 pM (RPMI-8226- Oct4 cells), 350 pM (MM-SP cells), and 1367 pM (RPMI-8226 cells), respectively. |
| Animal Protocol |
Animal/Disease Models: SCID-hu mice with INA-6 MM cells[1] Doses: 12 μg/kg, 16 μg/kg, 25 μg/kg and 50 μg/kg Route of Administration: intravenous (iv) injection; for 5 days each week for 3 weeks Experimental Results: Blocked pDC-induced tumor growth and prolonged mice survival at 12 μg/kg. demonstrated well tolerance at 16 μg/kg, while higher doses resulted in body weight decrease and toxicity. Animal/Disease Models: CB-17 mice with subcutaneous (sc) MM xenograft model[1] Doses: 16 μg/kg; with or without 2.5 mg/kg Pomalidomide (po; 4 days weekly for 2 weeks) Route of Administration: intravenous (iv) injection; dose at 5 days for first week Experimental Results: Enhanced the anti-MM activity of proteasome inhibitor and immunomodulatory drug pomalidomide. |
| References |
[1]. A novel agent SL-401 induces anti-myeloma activity by targeting plasmacytoid dendritic cells, osteoclastogenesis and cancer stem-like cells. Leukemia. 2017 Dec;31(12):2652-2660. |
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.) |