embalaje : 10mg
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Synonyms:
| Description | Deruxtecan is an ADC drug-linker conjugate composed of a derivative of DX-8951 (DXd) and a maleimide-GGFG peptide linker used in the synthesis of DS-8201 and U3-1402. |
| In vitro | METHODS: Trastuzumab Deruxtecan (DS-8201a) was administered at scalar concentrations of 0.005 μg/mL, 0.05 μg/mL, 0.2 μg/mL, 0.5 μg/mL, and 2.0 μg/mL. Three days after drug treatment, whole cells were harvested, centrifuged, and stained with propidium iodide (2 μl of 500 μg/mL stock solution in phosphate-buffered saline (PBS)). RESULTS DS-8201 induced cell death with a mean IC50 value of 0.03 μM (p<0.0001); statistically significant differences were observed in 3+ HER2/neu ovarian CS cell lines, where the mean IC50 of DS-8201a was 0.03 μM; and in representative HER2/neu non-expressing cell lines, where the mean IC50 of DS-8201a was 20.02 μM. [2] |
| In vivo | METHODS: Mouse models of HER2-positive tumors were treated with Trastuzumab Deruxtecan (DS-8201a) (10 mg/kg, i.v), and anti-PD-1 antibodies were also used in combination to evaluate synergistic effects, monitor tumor growth, and perform flow cytometric analysis. To analyze the composition and function of immune cells in tumors. RESULTS Trastuzumab Deruxtecan (DS-8201a) significantly inhibited tumor growth and in some cases resulted in complete remission (CR); mice that achieved CR after treatment were able to reject revaccinated CT26.WT-hHER2 cells as well as non-transgenic CT26.WT-mock cells, showing the formation of immune memory; Trastuzumab Deruxtecan (DS-8201a) increased the number of CD8+ T cells infiltrating within the tumor, upregulated the expression of CD86, an activation marker of dendritic cells (DCs), and enhanced Expression of PD-L1 and MHC class I molecules on tumor cells; the combination of Trastuzumab Deruxtecan (DS-8201a) and an anti-PD-1 antibody is more effective in inhibiting tumor growth than monotherapy, suggesting that Trastuzumab Deruxtecan (DS-8201a) may Promote anti-tumor immunity by activating the immune system and upregulating PD-L1 expression. [1] |
| Molecular Weight | 1034.05 |
| Formula | C52H56FN9O13 |
| Cas No. | 1599440-13-7 |
| Smiles | CC[C@@]1(O)C(=O)OCc2c1cc1-c3nc4cc(F)c(C)c5CC[C@H](NC(=O)COCNC(=O)CNC(=O)[C@H](Cc6ccccc6)NC(=O)CNC(=O)CNC(=O)CCCCCN6C(=O)C=CC6=O)c(c3Cn1c2=O)c45 |
| Relative Density. | 1.48 g/cm3 (Predicted) |
| Storage | Store at low temperature,Keep away from moisture Powder: -20°C for 3 years Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 262 mg/mL (253.37 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+90% Corn Oil: 2 mg/mL (1.93 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
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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