Payload · Topoisomerase I inhibitor

DXd

TopoI inhibitor

CC[C@@]1(C2=C(COC1=O)C(=O)N3CC4=C5[C@H](CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)NC(=O)CO)O

Physicochemistry

Properties

493.5 Da

XLogP3

logD₇.₄

1.4

TPSA

129 Å²

pKa

9.2

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Yes

PubChem CID

117888634

Bioactivity

Free DXd payload: TOP1 (DNA topoisomerase I) inhibitor; in vitro IC50 ~0.5 nM (MDA-MB-468) and ~4 nM (KPL-4) per ADCdb. T-DXd ADC IC50 0.7 ng/mL (SK-BR-3), 8.1 ng/mL (NCI-N87); cell-kill ranges ~0.7 to >3000 ng/mL by HER2 expression. Source: ADCdb PAY0UXDSB / DRG0ERKBH.

3 agents