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| ln Vitro |
Faziprumig (0.007-2000 pM; 48 hours) effectively induced redirected lysis, T cell activation, and cytokine release in a co-culture system of human peripheral blood mononuclear cells (PBMCs) and RAMOS cells. Its cytotoxicity and T cell activation EC50 values were all below the picomolar level. The presence of human serum albumin caused a slight change in the cytotoxic EC50 value, but did not prevent maximal cell lysis [1]. Faziprumig (0.007-2000 pM; 48 hours) effectively induced redirected lysis of A20 mouse lymphoma cells stably expressing human CD19, including clones with CD19 copy number as low as 325 per cell, accompanied by dose-dependent T cell activation and cytokine release. The cytotoxic EC50 value increased with decreasing CD19 density, but all tested clones achieved maximal cell lysis [1].
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| ln Vivo |
Faziprumig (0.1 mg/kg; intravenous injection; single dose) completely inhibited tumor growth of A20 lymphoma expressing human CD19 in BALB/c mice expressing hCD3ε[1]. Faziprumig (0.01–0.1 mg/kg; intravenous injection; once a week for 15 days) inhibited leukemia progression in NCG mice transplanted with Raji B.luc cells and human peripheral blood mononuclear cells (PBMCs)[1]. Faziprumig (0.3–30 µg/kg; intravenous/subcutaneous injection; once a week for 28 days) achieved 100% complete remission in NCG mice transplanted with Raji B.luc cells and human peripheral blood mononuclear cells (PBMCs), and all tested doses cleared human B cells and Raji cells from the peripheral blood[1].
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| Animal Protocol |
Animal/Disease Models:BALB/c mice expressing hCD3ε[1]
Doses: 0.1 mg/kg Route of Administration: Intravenous injection; single administration Experimental Results: Complete inhibition of tumor growth. Animal/Disease Models:NCG mice (immunodeficient) [1] Doses: 0.01, 0.03 and 0.1 mg/kg Route of Administration: Intravenous injection; once a week; 15 days Experimental Results: It prevented the increase of luciferase signaling, indicating that it inhibited the spread of leukemia. Animal/Disease Models:NCG mice (immunodeficient) [1] Doses: 0.3-30 µg/kg (intravenous, once weekly); 0.3-30 µg/kg (subcutaneous, once weekly) Route of Administration: Intravenous; once weekly; for 28 days; subcutaneous; once weekly; for 28 days Experimental Results: Complete remission (luciferase signal was comparable to background) was achieved at both 3 µg/kg and 30 µg/kg (intravenous or subcutaneous) doses. The 0.3 µg/kg (subcutaneous) dose had minimal effect, while the 0.3 µg/kg (intravenous) dose had moderate effect. Regardless of dose or route of administration, human B cells and Raji B.luc cells were depleted in peripheral blood in all treatment groups. |
| References |
| CAS # |
3059485-32-1
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| Appearance |
Typically exists as solids at room temperature
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| Synonyms |
CLN-978
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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.
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