Brenetafusp (10-13-10-8 M) can effectively activate T cells in a dose-dependent manner against HLA-A*02:01+ PRAME+ MEL624, MEWO, SKMEL5 and C32 melanoma cell lines, with EC50 values ranging from 12.4 to 98.0 pM[1]. Brenetafusp (10-14-10-9 M) can effectively mediate T cell-mediated cytotoxicity against HLA-A*02:01+ PRAME+ MEL624, MEWO and C32 melanoma cell lines, with EC50 values ranging from 2.99 to 20.4 pM[1]. Brenetafusp (10-13-10-8 M) can effectively activate T cells in a dose-dependent manner to combat HLA-A*02:01+ PRAME+ NCI-H1755 and NCI-H1703 non-small cell lung cancer (NSCLC) cell lines, with EC50 values of 17.9 pM and 76.9 pM, respectively[1]. Brenetafusp (10-14-10-9 M) can effectively mediate the cytotoxicity of T cells against HLA-A*02:01+ PRAME+ NCI-H1755 and NCI-H1703 non-small cell lung cancer (NSCLC) cell lines, with EC50 values of 1.3 pM and 4.4 pM, respectively[1]. Brenetafusp (10-13-10-8 M) can effectively activate T cells in a dose-dependent manner to combat HLA-A*02:01+ PRAME+ OV56 and COV318 ovarian cancer cell lines, with EC50 values of 2.4 pM and 17.4 pM, respectively[1]. Brenetafusp (10-14-10-9 M) can effectively mediate T cell-mediated cytotoxicity against HLA-A*02:01+ PRAME+ OV56 and COV318 ovarian cancer cell lines, with EC50 values of 1.6 pM and 10.5 pM, respectively[1]. Brenetafusp (10-1000 pM) can effectively guide T cells to induce dose-dependent apoptosis in tumor organoids derived from HLA-A*02:01+ PRAME+ patients[1]. Brenetafusp (10-13-10-8 M)-mediated T cell activation depends on the expression of PRAME in MEL624 melanoma cells. It has significant activity in parental cells, reduced activity in PRAME knockout cells, and dose-dependent recovery of activity in knockout cells with restored PRAME expression [1]. Brenetafusp (10-100 pM; 80 hours) can redirect PD-1+ depleted tumor-infiltrating lymphocytes (TILs) to kill PD-L1+ MEL624 melanoma cells, but its activity is impaired, while anti-PD-1 antibodies can completely restore its activity [1]. Brenetafusp (concentrations up to 10 nM for bronchial epithelial cells and down to 1 nM for melanocytes) has very low responsiveness to primary normal human bronchial epithelial cells and melanocytes, indicating that it is specific to PRAME+ tumor cells [1].

Cytotoxicity assay [1]
Cell Types: PD-1+ and PD-1- tumor-infiltrating lymphocytes (TILs) from melanoma biopsies, co-cultured with PD-L1+ or PD-L1- MEL624 melanoma cells
Tested Concentrations: 10 pM, 100 pM
Incubation Duration: 80 hours
Experimental Results: At a concentration of 100 pM, PD-1+ TILs were 3-10 times less cytotoxic to PD-L1+ MEL624 cells than to PD-L1- cells; co-incubation with anti-PD-1 antibody completely restored this cytotoxicity.

[1]. High-affinity T cell receptor ImmTAC® bispecific efficiently redirects T cells to kill tumor cells expressing the cancer-testis antigen PRAME. Immunother Adv. 2024;4(1):ltae008. Published 2024 Nov 2.

2736407-54-6

Colorless to light yellow liquid

IMC-F106C

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

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

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.

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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).

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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)

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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).

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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

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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.

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 (Please use freshly prepared in vivo formulations for optimal results.)