Products Description
English name：Dxd is an inhibitor antibody binding drug
CAS number：1599440-33-1
Molecular formula C26H24FN3O6
Molecular weight 493.48
Molecular structure:
Related categories of cytotoxins; Standard products; Biological reagent; Chemical reagent
Derivative properties of DX-8951
Boiling point 957.9±65.0 °C(Predicted)
Density 1.57± 0.1g /cm3(Predicted)
Store at -20°C
Solubility DMSO:40.0(Max concentration mg/mL); 81.06(Max concentration mM)
Morphological solid
Acidity coefficient (pKa)11.18±0.40(Predicted)
Use and synthesis of DX-8951 derivatives
Biological activity
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor with IC50 of 0.31 μM. Payload of an antibody-coupled drug ADC (DS-8201a) that can be used to target HER2.
Target spot
Topoisomerase I 0.31 μM (IC 50 ) Camptothecins
In vitro study
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC 50 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 IC 50 s 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 IC 50 values of 26.8, 25.4, and 6.7 ng/mL, respectively, but with no such inhibition on MDA-MB-468 (IC 50 , >10,000 ng/mL).
In vivo study
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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