Dxd 是一种有效的DNA 拓扑异构酶 I 抑制剂，IC50值为 0.31 μM，用作HER2靶向ADC的偶联药物。

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.

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].

1599440-33-1

C26H24FN3O6

493.48

UNII-OQM5SD32BQ;Exatecan derivative for ADC;OQM5SD32BQ

H2O:insoluble
DMSO:50 mg/mL (101.32 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years