Physicochemical Properties
| CAS # | 1646327-65-2 |
| 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 | EC50 for binding activity: 0.34 μg/mL(Ramos cells); 0.47 μg/mL(Raji cells); 0.74 μg/mL(ARH-77 cells); 0.37 μg/mL(FcyRIIIa-Val158 transfected cells); 1.18 μg/mL(FcyRIIIaPhe158 transfected cells)[1] |
| ln Vitro | For Ramos, Raji, and ARH-77 cells, MDX-1342 (0-100 μg/mL; 30 min) exhibits binding activity with EC50 values of 0.34, 0.47, and 0.74 μg/mL, respectively[1]. For FcyRIIIa-Val158 and FcyRIIIaPhe158 transfected cells, MDX-1342 (0-100 μg/mL; 30 min) exhibits binding activity with EC50 values of 0.37 and 1.18 μg/mL, respectively[1]. The antibody-dependent cellular cytotoxicity (ADCC) of MDX-1342 (0-100 μg/mL) is strong, with a typical EC50 value of 0.01-0.02 ug/mL[1]. Macrophages phagocytose ARH-77 cells in a dose-dependent manner with the use of MDX-1342 (0-100 μg/mL)[1]. |
| ln Vivo | Using a mouse B-cell lymphoma model, MDX-1342 (iv; 0.03, 0.3, 3 and 30 mg/kg; 200 μL) exhibits dose-dependent increase in survival[1]. In vivo, MDX-1342 (iv; 0.1 or 1 mg/kg; single) exhibits strong B-cell depletion, enhances affinity for cynomolgus monkey FcyRllla, and binds to cynomolgus monkey CD19 at a low nanomolar concentration[1]. |
| Cell Assay |
Cell Viability Assay[1] Cell Types: human CD19-transfected CHO cells Tested Concentrations: 0-100 μg/mL Incubation Duration: 30 min Experimental Results: demonstrated increased affinity for FcyRIlla-Phe158 and FcyRIlla-Val158 receptors. |
| Animal Protocol |
Animal/Disease Models: cynomolgus monkey[1] Doses: 0.1 or 1 mg/kg Route of Administration: iv, single Experimental Results: demonstrated B-cell depletion in the cynomolgus monkey. Animal/Disease Models: Ramos systemic tumor xenograft model(SCID mice)[1] Doses: 0.03, 0.3, 3 and 30 mg/kg Route of Administration: iv, 200 μL Experimental Results: demonstrated dose-dependent improvement in survival. |
| References | [1]. Pina M Cardarelli, et al. A nonfucosylated human antibody to CD19 with potent B-cell depletive activity for therapy of B-cell malignancies. Cancer Immunol Immunother. 2010 Feb;59(2):257-65. |
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.) |