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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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
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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.