| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
This agent simultaneously targets two distinct immunosuppressive pathways: (1) PD-L1, via its antibody domain, which blocks the PD-1/PD-L1 interaction, and (2) TGF-beta, via its TGF-betaRII trap domain, which neutralizes TGF-beta ligands in the tumor microenvironment. It is designed to unleash an anti-tumor immune response while preventing immune evasion.
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| ln Vitro |
Long-term protective immunity can be conferred by bintrafusp alfa, which can also decrease regulatory T cell activity, greatly increase the infiltration of CD8+ T cells and natural killer cells, and decrease the infiltration of intratumoral bone marrow-derived suppressor cells [1].
In vitro, Bintrafusp alfa can confer long-term protective immunity. It reduces regulatory T cell (Treg) function, significantly increases the infiltration of CD8+ T cells and Natural Killer (NK) cells into tumors, and reduces the infiltration of intratumoral myeloid-derived suppressor cells (MDSCs), thereby shifting the tumor microenvironment from an immunosuppressive to a pro-inflammatory state. |
| ln Vivo |
In animal models, Bintrafusp alfa demonstrates superior antitumor activity compared to anti-PD-L1 monotherapy. By blocking both checkpoints, it can reduce Treg function and increase CD8+ T cell and NK cell infiltration into tumors, leading to potent and durable tumor regression and the establishment of immunological memory.
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| Enzyme Assay |
Cell-free binding assays use a Biacore system. The PD-L1 binding affinity is measured by immobilizing recombinant human PD-L1 and flowing Bintrafusp alfa over the chip. For TGF-beta binding, the ‘trap‘ domain is assayed for its ability to bind to TGF-beta1, -beta2, and -beta3 isoforms using surface plasmon resonance (SPR) to determine the equilibrium dissociation constants (KD).
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| Cell Assay |
Cellular assays use mixed lymphocyte reactions or cancer cell lines co-cultured with immune cells. Bintrafusp alfa is added to the culture. Reporter cell lines for PD-1/PD-L1 blockade (e.g., Jurkat T cells expressing PD-1) are used to quantify checkpoint inhibition. T cell activation is measured by IL-2 production or CD69 expression via flow cytometry.
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| Animal Protocol |
Animal studies are conducted in syngeneic mouse tumor models (e.g., EMT-6 breast cancer, CT26 colon cancer). Mice are treated with Bintrafusp alfa via intraperitoneal injection. Tumor growth is monitored. At the end of the study, tumors are harvested for immune profiling by flow cytometry (e.g., CD8+ T cells, Tregs, MDSCs) and for gene expression analysis of T cell-related markers.
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) profile of Bintrafusp alfa is characteristic of a monoclonal antibody fusion protein, with a long half-life that supports infrequent dosing. It is administered intravenously. The fusion protein has a molecular weight of approximately 360 kDa, and its size contributes to a limited volume of distribution and slow systemic clearance.
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| Toxicity/Toxicokinetics |
Bintrafusp alfa has been investigated in clinical trials (Phase I-III) for various solid tumors. The most common treatment-related adverse events are typically rash, pruritus, fatigue, and gastrointestinal issues. The dual mechanism has not shown a distinct safety signal beyond those associated with either PD-1/PD-L1 or TGF-beta blockade alone.
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| References | |
| Additional Infomation |
Bintrafusp alfa was investigated in clinical trials for advanced solid tumors, including biliary tract cancer, NSCLC, and HPV-associated cancers. Although its clinical development program was discontinued by the sponsor in 2021, it remains a valuable research tool for understanding the biology of dual pathway blockade. It serves as a benchmark for next-generation bispecific approaches.
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| CAS # |
1918149-01-5
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| Appearance |
Colorless to light yellow liquid
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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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