Sacituzumab
Sacituzumab Basic information
- Product Name:
- Sacituzumab
- Synonyms:
-
- Sacituzumab
- Research Grade Sacituzumab(DHC43301)
- Sacituzumab (anti-TROP2)
- Sacituzumab|||Sacituzumab (anti-Trop-2)
- Research Grade Sacituzumab
- (2R)-2-amino-3-[1-[[4-[[1-[2-[2-[2-[2-[2-[2-[2-[2-[2-[[2-[2-[[(2S)-6-amino-1-[4-[[(19S)-10,19-diethyl-7-hydroxy-14,18-dioxo-17-oxa-3,13-diazapentacyclo[11.8.0.02,11.04,9.015,20]henicosa-1(21),2,4(9),5,7,10,15(20)-heptaen-19-yl]oxycarbonyloxymethyl]anilino]-1-oxohexan-2-yl]amino]-2-oxoethoxy]acetyl]amino]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethoxy]ethyl]triazol-4-yl]methylcarbamoyl]cyclohexyl]methyl]-2,5-dioxopyrrolidin-3-yl]sulfanylpropanoic acid
- CAS:
- 1796566-95-4
- MW:
- 0
- Mol File:
- Mol File
Sacituzumab Chemical Properties
- form
- Liquid
- color
- Colorless to light yellow
Sacituzumab Usage And Synthesis
Uses
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].
in vivo
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].
| Animal Model: | MDA-MB-468 xenograft model of 6-week-old female BALB/c nude mice[1] |
| Dosage: | 50 mg/kg |
| Administration: | i.v., intervals of 5 days and repeated a total of four times |
| Result: | Decreased the tumor inhibition rate to 29.1% at 50 mg/kg in MDA-MB-468 xenograft model. |
References
[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. DOI:10.1016/j.ijbiomac.2023.127105
[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. DOI:10.1016/j.isci.2021.103190
[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. PMID:7493360
[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. DOI:10.1016/j.annonc.2021.06.002
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