Sacituzumab 

Sacituzumab is a humanized IgG1 monoclonal antibody targeting Trophoblast cell surface antigen 2 (TROP2). Sacituzumab demonstrates a lack of antitumor effects alone and does not inhibit the function of TROP-2 during tumor metastasis, binding to the linear epitopes of TROP-2 protein. Sacituzumab is used for the synthesis of antibody-drug conjugates (ADC) drugs. Antibody-drug conjugates with sacituzumab (sacituzumab govitecan) (HY-132254) targeting TROP-2 have been approved for the field of triple-negative breast cancer^[1][2][3][4].

Human IgG1 kappa

Human IgG1 kappa, Isotype Control

Humanized

Sacituzumab (0.5 nM, 800 s) possesses non-competitive binding sites and recognized distinct epitopes of TROP-2 on the antigen. Additionally, the binding to cancer cell lines activities of Sacituzumab and hIMB1636 is similar^[1].
Sacituzumab (5 mg/mL, 48 h) binds to a linear epitope within TROP-2, which might not interrupt the assembly of TROP-2 molecules on the cell surface in HEK-293T cells^[2].

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

Sacituzumab (50 mg/kg, i.v., every 5 days for four times) exhibits a weak antitumor effect without significant weight loss in MDA-MB-468 xenograft mouse model^[1].

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

1796566-95-4

Liquid

Colorless to light yellow

[Sacituzumab]

Shipping with dry ice.

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

• 
  Human IgG1 kappa

• 
  Loaded TROP-2 Protein, Human (248a.a, HEK293, His, HY-P70457) on AHC2 biosensor, can bind Sacituzumab with an affinity constant of 8.077E-10 M as determined in BLI assay.
• 
  Flow cytometry analysis of Trop2 overexpression HEK293 cells labelling Trop2 with Sacituzumab at 67nM (Red). Goat anti human IgG Fc (Alexa Fluor488) was used as the secondary antibody at 1/400 dilution. Isotype control - human IgG (Blue). Unlabeled control - Unlabelled cells (Gray).
• 
  Immobilized TROP-2 Protein, Human (HY-P70457) can bind Sacituzumab, with the EC₅₀ is 1.335 ng/mL.

• [1]. Zhou DD, et al. Elucidating the development, characterization, and antitumor potential of a novel humanized antibody against Trop2[J]. Int J Biol Macromol. 2023 Dec 31;253(Pt 6):127105.  [Content Brief]

  [2]. Sun M, et al. Structural insights into the cis and trans assembly of human trophoblast cell surface antigen 2[J]. iScience. 2021 Sep 30;24(10):103190.  [Content Brief]

  [3]. Shih LB, et al. In vitro and in vivo reactivity of an internalizing antibody, RS7, with human breast cancer[J]. Cancer Res. 1995 Dec 1;55(23 Suppl):5857s-5863s.  [Content Brief]

  [4]. Bardia A, et al. Biomarker analyses in the phase III ASCENT study of sacituzumab govitecan versus chemotherapy in patients with metastatic triple-negative breast cancer. Ann Oncol. 2021 Sep;32(9):1148-1156.  [Content Brief]