Dxd is a potent inhibitor of DNA topoisomerase I with an IC50 of 0.31 μM. It is used as a conjugated drug of HER2-targeting ADC. 

Topoisomerase I    Camptothecins  

Dxd shows obviously suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines with IC50s of 26.8, 25.4, and 6.7 ng/mL respectively, but with no such inhibition on MDA-MB-468 (IC50, >10,000 ng/mL)[1]. 

Dxd is cytotoxic to human cancer cell lines of KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50s of 1.43 nM-4.07 nM. In HER2 low-expressing ST565 and ST313 models has HER2 IHC 1+/FISH-negative expression[1].

Exatecan derivative for ADC , 化合物Dxd

98%

493.48 

C₂₆H₂₄FN₃O₆

1. Ogitani Y, et al. DS-8201a, A Novel HER2-Targeting ADC with a Novel DNA Topoisomerase I Inhibitor, Demonstrates a Promising Antitumor Efficacy with Differentiation from T-DM1. Clin Cancer Res. 2016 Oct 15;22(20):5097-5108.

For research use only .