Reagentia en instrumenten voor immunologie, celbiologie en moleculaire biologie.

Deruxtecan [1599440-13-7]

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Referentie NB-64-06389-10mg

Formaat : 10mg

Merk : Neo Biotech

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Deruxtecan

(Synonyms: MC-GGFG-Dxd) Copy Product Info

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Synonyms: MC-GGFG-Dxd

Catalog No. T15098 Copy Product Info

Purity: 99.95%

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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.

Cas No. 1599440-13-7

With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.

For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.95%

Appearance:Solid

Color:White to Yellow

Product Information

Bioactivity

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]
Synonyms	MC-GGFG-Dxd

Chemical Properties

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 & Solubility Information

Storage

Keep away from moisture,Keep away from direct sunlight,Store under nitrogen,Store at low temperature,The compound is unstable in solution. Please use soon, 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

	1mg	5mg	10mg	50mg
1 mM	0.9671 mL	4.8354 mL	9.6707 mL	48.3536 mL
5 mM	0.1934 mL	0.9671 mL	1.9341 mL	9.6707 mL
10 mM	0.0967 mL	0.4835 mL	0.9671 mL	4.8354 mL
20 mM	0.0484 mL	0.2418 mL	0.4835 mL	2.4177 mL
50 mM	0.0193 mL	0.0967 mL	0.1934 mL	0.9671 mL
100 mM	0.0097 mL	0.0484 mL	0.0967 mL	0.4835 mL

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.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

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.

Stock Solution Preparation:

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.

Preparation of the In Vivo Formulation:

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.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

InhibitorinhibitDrugLinkerConjugatesforADCDrug-Linker Conjugates for ADCDrugLinker Conjugates for ADCDeruxtecanCamptothecins

Related Tags: Deruxtecan chemical structure | Deruxtecan in vivo | Deruxtecan in vitro | Deruxtecan formula | Deruxtecan molecular weight