| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| ln Vitro |
RG-6333 (RO 7443904) has a low affinity for CD28 in CHO cells (Kd: 36 nM), and the binding is weak but sufficient to provide a co-stimulatory signal [1]. RG-6333 is inactive as a single drug in human peripheral blood mononuclear cells (PBMCs) and can only activate T cells after binding to the T cell receptor (TCR) [1].
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| ln Vivo |
RG-6333 (1.10 mg/kg, single intravenous injection) activates T cells only in the presence of T cell receptor (TCR) signaling in humanized NSG mice and does not induce cytokine storm [1][2]. RG-6333 (1 mg/kg, single intravenous injection) in combination with Glofitamab (0.15 mg/kg) significantly inhibited tumor growth in humanized NSG mice subcutaneously inoculated with NALM-6 lymphoma and increased tumor-infiltrating CD8+ T cells [1]. In a humanized mouse model of invasive in vivo lymphoma (DLBCL WSU-DLCL2-Fluc), RG-6333 (1 mg/kg, single intravenous injection) in combination with Glofitamab (0.15 mg/kg) resulted in complete tumor regression, with an initial transient weight loss due to T cell activation, followed by weight recovery [1][2]. In a humanized NSG mouse model carrying subcutaneous OCI-Ly18 tumors, the combined use of RG-6333 (1 mg/kg, once intravenously) and glofitamab (0.15 mg/kg) increased the signature of pro-inflammatory T cells in the tumor and promoted transendothelial migration, while the triple combination with CD19-4-1BBL deepened and prolonged the in vivo antitumor response [1].
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| Animal Protocol |
Animal/Disease Models:Humanized NSG mice carrying orthotopic WSU-DLCL2-Fluc tumors [1]
Doses: 1 mg/kg Route of Administration: Intravenous injection, three-dose combination Therapeutic Experimental Results: Combined administration with Glofitamab (0.15 mg/kg) achieved complete tumor regression. Initially, mice showed weight loss, which is related to the mechanism of action of TCB and the release of cytokines it induces. After combined administration with Glofitamab (0.15 mg/kg), the mice returned to normal and did not show further weight loss, indicating that the tumor did not progress, suggesting that TCB has strong anti-tumor activity. Animal/Disease Models:Tumor-bearing humanized NSG mice [1] Doses:1 mg/kg< Route of Administration:Intravenous injection, three-dose combination Experimental Experimental Results:Combined administration with Glofitamab (1 mg/kg) increased the count of CD8+ and CD4+ T cells in the tumor. Combined administration with Glofitamab (1 mg/kg) significantly increased the expression of IFNγ pathway genes, followed by a significant increase in cytotoxic T cells and a significant decrease in B cell characteristics. Combined administration with Glofitamab (1 mg/kg) and CD19-4-1BBL (1 mg/kg) prolonged the in vivo anti-tumor response and achieved long-term tumor control. |
| References |
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| Appearance |
Colorless to light yellow liquid
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| Synonyms |
RO7443904
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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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