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Dxd

CAS No. : 1599440-33-1

產(chǎn)品活性：Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC₅₀ of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).

研究領(lǐng)域：Cell Cycle/DNA Damage  |  Antibody-drug Conjugate/ADC Related

作用靶點(diǎn)：Topoisomerase  |  ADC Cytotoxin

In Vitro: Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC₅₀ of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a). 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, but the control IgG-ADC (Dxd is the payload) shows no inhibition on the four cell lines (with HER2 expression). DS-8201a (Dxd is the payload) displays significant suppression on the HER2-positive KPL-4, NCI-N87, and SK-BR-3 cell lines, with IC₅₀ values 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).

In Vivo: DS-8201a (Dxd is the payload, 10 mg/kg, i.v.) shows potent antitumor activity in HER2-positive models with KPL4, JIMT-1, and Capan-1 and in HER2 low-expressing ST565 and ST313 models with HER2 IHC 1+/FISH-negative expression.

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