vadastuximab talirine   Click here for help

GtoPdb Ligand ID: 9434

Synonyms: SGN-CD33A
Immunopharmacology Ligand
Compound class: Antibody
Comment: Vadastuximab talirine (SGN-CD33A; Seattle Genetics) is an humanized anti-CD33 antibody-drug conjugate (ADC) which delivers a toxic payload to CD33 +ve cells [1]. Talirine is a pyrrolobenzodiazepine (PBD) dimer (PubChem CID 45257190), which is a DNA crosslinking agent, causing DNA damage and ultimately apoptosis of targeted cells. Talirine is conjugated to engineered Cys residues in the antibody via a cathepsine B cleavable linker.
Annotated peptide sequences for this antibody are available from its IMGT/mAb-DB record.
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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
Preclinically SGN-CD33A proved more potent than the approved anti-CD33 mAb gemtuzumab ozogamicin, against a panel of AML cell lines and primary AML cells in vitro and in vivo, including efficacy against multidrug-resistant cells [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
CD33 Primary target of this compound Hs Antibody Binding 9.3 pKd - 1
⤷ pKd 9.3 (Kd 5x10-10 M) [1]
Description: Saturation binding in HEL 92.1.7 cells endogenously expressing human CD33.