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Dxd

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Catalog No. T11249LCas No. 1599440-33-1
Alias UNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADC

Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.

Dxd

Dxd

🥰Excellent
Purity: 100%
Catalog No. T11249LAlias UNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADCCas No. 1599440-33-1
Dxd (OQM5SD32BQ) is a potent DNA topoisomerase I inhibitor (IC50= 0.31 μM). Dxd was used as a conjugate drug for HER2-targeted ADCs.
Pack SizePriceAvailabilityQuantity
1 mg$39In Stock
5 mg$68In Stock
10 mg$97In Stock
25 mg$159In Stock
50 mg$233In Stock
1 mL x 10 mM (in DMSO)$74In Stock
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Purity:100%
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Product Introduction

Bioactivity
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.
Targets&IC50
SK-BR-3 cells:6.7 ng/mL, Topo I:0.31 μM, KPL-4 cells:26.8 ng/mL, NCI-N87 cells:25.4 ng/mL, MDA-MB-468 cells:> 10,000 ng/mL
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]
SynonymsUNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADC
Chemical Properties
Molecular Weight493.48
FormulaC26H24FN3O6
Cas No.1599440-33-1
SmilesCC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cc(F)c(C)c5CC[C@H](NC(=O)CO)c(c3Cn1c2=O)c45
Relative Density.1.57 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -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: 50 mg/mL (101.32 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.0264 mL10.1321 mL20.2642 mL101.3212 mL
5 mM0.4053 mL2.0264 mL4.0528 mL20.2642 mL
10 mM0.2026 mL1.0132 mL2.0264 mL10.1321 mL
20 mM0.1013 mL0.5066 mL1.0132 mL5.0661 mL
50 mM0.0405 mL0.2026 mL0.4053 mL2.0264 mL
100 mM0.0203 mL0.1013 mL0.2026 mL1.0132 mL

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