Dxd

SKU: orb1309686

Description

Dxd

Research Area

Molecular Biology

Key Properties

• CAS Number: 1599440-33-1
• MW: 493.48
• Purity: 99.85% (May vary between batches)
• Formula: C₂₆H₂₄FN₃O₆
• SMILES: CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cc(F)c(C)c5CC[C@H](NC(=O)CO)c(c3Cn1c2=O)c45
• Target: Topoisomerase|||ADC Cytotoxin
• Solubility: H2O:insoluble;DMSO:51.5 mg/mL (104.36 mM)

Bioactivity

• Target IC50:
  NCI-N87 cells:25.4 ng/mL|SKBR3 cells:6.7 ng/mL|MDA-MB-468 cells:> 10,000 ng/mL|KPL-4 cells:26.8 ng/mL|Topo I:0.31 μM
• 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.
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• 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).
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Dxd, ADC Cytotoxin, ADC, ADCCytotoxin, ADC Payload, Camptothecins, inhibit, Inhibitor, OQM5SD32BQ, Exatecan derivative for ADC, HER2-targeting, Topoisomerase, Topoisomerase I, UNII-OQM5SD32BQ

Compound Identifiers

PubChem CID

117888634