Payload · Topoisomerase I inhibitor

Rezetecan (SHR9265 / SHR169265)

TopoI inhibitor

CCC1(C2=C(COC1=O)C(=O)N3CC4=C5C(CCC6=C5C(=CC(=C6C)F)N=C4C3=C2)NC(=O)C(C7CC7)O)O

Physicochemistry

Properties

533.55 Da

XLogP3

3.67

logD₇.₄

1.89

TPSA

129 Å²

pKa

Charge pH 7.4

H-bond donors

H-bond acceptors

Bystander

Yes

PubChem CID

172874939

Bioactivity

Payload SHR9265/SHR169265 is a DNA topoisomerase I (TOP1) inhibitor (exatecan-derived camptothecin; TOP1 inhibition comparable to SHR167971/DXd-class). ADC SHR-A1811 (DAR ~6) cytotoxicity IC50 0.3-2.32 nM across nine cancer cell lines; bystander killing IC50 0.23 +/- 0.05 nM on H

1 agent