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sacituzumab tirumotecan   Click here for help

GtoPdb Ligand ID: 13791

Synonyms: Jiataile® | MK-2870 | sac-TMT | SKB-264 | SKB264
Approved drug
sacituzumab tirumotecan is an approved drug
Compound class: Antibody
Comment: Sacituzumab tirumotecan (SKB264/MK-2870) is an antibody-drug conjugate (ADC) [1-2]. It is the same humanized anti-TROP-2 monoclonal antibody as the previously approved ADC sacituzumab govitecan, but carrying a different topoisomerase inhibitor payload (tirumotecan/KL610023) that is a belotecan-derivative. TROP-2 is a transmembrane glycoprotein, cell surface antigen which has oncogenic activity in cancers of epithelial origin [6], but expression is restricted in normal tissue. Directing the topoisomerase inhibitor selectively to cancer cells via TROP-2 binding is predicted to limit toxicity towards healthy tissue/cells.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
Bioactivity Comments
The intracellularly-cleaved toxic payload causes cell cycle arrest at the G2/S stage and death of TROP2 +ve cells. The anti-proliferative IC50 of tirumotecan/KL610023 in HCC1806 cells is 1.8 nM [1].
Selectivity at other protein targets
Key to terms and symbols Click column headers to sort
Target Sp. Type Action Value Parameter Concentration range (M) Reference
tumor associated calcium signal transducer 2 Hs Antibody Binding 9.5 pKd - 1
⤷ pKd 9.5 (Kd 3.1x10-10 M) [1]
Description: Binding affinity determined by SPR