Payload · Topoisomerase I inhibitor

Exatecan

TopoI inhibitor

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

Physicochemistry

Properties

435.4 Da

XLogP3

0.4

logD₇.₄

TPSA

106 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Yes

PubChem CID

151115

Bioactivity

Payload exatecan (DX-8951f) is a potent DNA topoisomerase I (TOP1) inhibitor; reported cell-free/enzymatic IC50 ~2.2 uM (0.975 ug/mL) with strong membrane permeability and bystander effect. ADC: FRalpha-directed, homogeneous DAR 8; sesutecan is a hydrophilic, stable, cleavable ex

4 agents