Tebentafusp  (Synonyms: IMCgp100)

Tebentafusp (IMCgp100) is a bispecific fusion protein to target gp100 peptide-HLA-A*02:01 (a melanoma-associated antigen). Tebentafusp guides T cells to kill gp100-expressing tumor cells via a high affinity T-cell receptor (TCR) binding domain and an anti-CD3 T-cell engaging domain. Tebentafusp leads to inflammatory cytokines and cytolytic proteins production, resulting in the direct lysis of tumour cells^[1][2].

scFv-kappa-heavy-TR-BETA-2_TR-ALPHA

Human

CD3E & PMEL

Tebentafusp is an ImmTAC recognizing a peptide derived from the melanoma-specific protein, gp100, presented by HLA-A*0201^[3].
Tebentafusp (31 pM, 82 pM, and 131 pM; 16 h) stimulates cytotoxic degranulation activity of PBMC against Mel526 cells rather than gp100-negative A375 cells^[3].
Tebentafusp (100 pM; 0-50 h) mediates CD8⁺ T cell killing despite the presence of regulatory T cells via monitoring caspase 3/7 activation during 40-48 hr^[3].
Tebentafusp (100 pM; 0-80 h) triggers cytolysis of melanoma cells by CD4⁺ T cell subpopulations^[3].
Tebentafusp (1, 12, 31, 82, and 131 pM; 24 h or 96 h) increases granzyme B amount, and induces broad cytokine and chemokine release including in both CD4⁺ and CD8⁺ cells^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tebentafusp (10 μg/kg; i.v.) inhibits tumor growth in mouse melanoma model^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

916  [NCBI] & 6490  [NCBI]

P07766 & P40967

ELISA, FACS, Functional assay

Unconjugated

The product can be reconstituted/diluted with sterile PBS or saline.

76.16 kDa

1874157-95-5

Liquid

Colorless to light yellow

[Tebentafusp]

Shipping with dry ice.

Please refer to the lot-specific COA for specific buffer information.

Please store the product under the recommended conditions in the Certificate of Analysis.

• 
  scFv-TR-Alpha_Beta-2

• 
  Loaded HLA-A*0201 GP100 Complex Protein, Human (Biotinylated, YLEPGPVTA, HEK293, His-Avi, HY-P77754) on NTA biosensor, can bind Tebentafusp with an affinity constant of 7.761E-10 M as determined in BLI assay.
• 
  Flow cytometric analysis of 1×10⁶ Jurkat cells labelling CD3E (red) with Tebentafusp (HY-P99339). Cells were fixed with 4% paraformaldehyde and permeabilised with 90% methanol. Then stained with the primary antibody at 1/200 dilution for an hour at 4℃. Alexa Goat Anti-Human IgG H&L (AF488) (HY-P83776) was used as the secondary antibody at 1/1,000 dilution for 30 minutes at 4℃. Human IgG1 kappa Isotype Control (HY-P99001, blue) was used as the isotype control.

• [1]. Middleton MR, et al. Tebentafusp, A TCR/Anti-CD3 Bispecific Fusion Protein Targeting gp100, Potently Activated Antitumor Immune Responses in Patients with Metastatic Melanoma. Clin Cancer Res. 2020 Nov 15;26(22):5869-5878.  [Content Brief]

  [2]. Dhillon S. Tebentafusp: First Approval. Drugs. 2022 Apr;82(6):703-710.  [Content Brief]

  [3]. Boudousquie C, et al. Polyfunctional response by ImmTAC (IMCgp100) redirected CD8+ and CD4+ T cells. Immunology. 2017 Nov;152(3):425-438.  [Content Brief]

  [4]. Baeuerle P A, et al. Passive immunotherapy by T cell–engaging bispecifi c antibodies[M]//Cancer Vaccines. CRC Press, 2015: 266-278.