embalaje : 10mg
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Synonyms: UNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADC
| 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 | MDA-MB-468 cells:> 10,000 ng/mL, SKBR3 cells:6.7 ng/mL, Topo I:0.31 μM, NCI-N87 cells:25.4 ng/mL, KPL-4 cells:26.8 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] |
| Synonyms | UNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADC |
| Molecular Weight | 493.484 |
| Formula | C26H24FN3O6 |
| Cas No. | 1599440-33-1 |
| Smiles | O=C1C2=C([C@@](O)(CC)C(OC2)=O)C=C3C4=NC5=CC(F)=C(C)C6=C5C([C@H](CC6)NC(CO)=O)=C4CN13 |
| Relative Density. | 1.57 g/cm3 (Predicted) |
| Storage | Keep away from direct sunlight 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: 51.50 mg/mL (104.36 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
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