| Name | Dxd |
| Description | Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs. |
| In vitro | METHODS: Human cancer cell lines KPL-4, NCI-N87, SK-BR-3 and MDA-MB-468, HER2-positive KPL-4, NCI-N87 and SK-BR-3 cell lines, and MDA-MB-468 cell lines were treated with Dxd for 6 days. Cell viability was measured using CellTiter-Glo luminescent cell viability assay reagent.
RESULTS: Dxd showed cytotoxicity against human cancer cell lines KPL-4, NCI-N87, SK-BR-3, and MDA-MB-468 with IC50 of 1.43 nm-4.07 nM ng/mL. Dxd significantly inhibited HER2 positive KPL-4, NCI-N87 and SK-BR-3 cell lines with IC50 of 26.8, 25.4 and 6.7 ng/mL, respectively. However, no such inhibitory effect was observed in MDA-MB-468 cells treated with Dxd (IC50 >10000 ng/mL). [1] |
| In vivo | METHODS: To investigate the antitumor activity of Dxd, DS-8201a (Dxd as payload) (10 mg/kg) was injected intravenously in a HER2-positive mouse model with KPL4, JIMT-1, and Capan-1 and in HER2 low expression ST565 vs Mouse model of ST313 with a single injection.
RESULTS: Dxd showed potent antitumor activity. [1] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | H2O : insoluble
DMSO : 51.5 mg/mL (104.36 mM), Sonication is recommended.
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| Keywords | Topoisomerase I | Topoisomerase | Inhibitor | inhibit | HER2-targeting | Dxd | Camptothecins | ADCCytotoxin | ADC Payload | ADC Cytotoxin | ADC |
| Inhibitors Related | Ciprofloxacin hydrochloride monohydrate | Levofloxacin hydrochloride | Norfloxacin | Anthraquinone | Methotrexate disodium | Prulifloxacin | 1,4-Naphthoquinone | Ofloxacin | Levofloxacin | Dexamethasone | 3-Hydroxypyridine | Etoposide |
| Related Compound Libraries | DNA Damage & Repair Compound Library | Bioactive Compound Library | Inhibitor Library | Anti-Aging Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
