Dxd

Research use only, not for human use.

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 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.(In Vitro):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).(In Vivo):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.

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).

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.

Exatecan derivative for ADC | OQM5SD32BQ | UNII-OQM5SD32BQ

Cell Cycle/DNA Damage

Topoisomerase

α-adrenergic receptor

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1599440-33-1

493.491

C26H24FN3O6

>98% (HPLC)

In Vitro:?DMSO : 40 mg/mL (81.06 mM)

CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cc(F)c(C)c5CC[C@H](NC(=O)CO)c(c3Cn1c2=O)c45

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(-20℃)

With Ice Pack

≥ 2 years