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Dxd [1599440-33-1]

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Référence NB-64-02516-10mg

Conditionnement : 10mg

Marque : Neo Biotech

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Dxd

(Synonyms: UNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADC) Copy Product Info

Synonyms: UNII-OQM5SD32BQ, OQM5SD32BQ, Exatecan derivative for ADC

Catalog No. T11249L Copy Product Info

Purity: 99.85%

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

Cas No. 1599440-33-1

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:99.85%

Appearance:Solid

Color:White to Yellow

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	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

Chemical Properties

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 & Solubility Information

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

	1mg	5mg	10mg	50mg
1 mM	2.0264 mL	10.1320 mL	20.2641 mL	101.3204 mL
5 mM	0.4053 mL	2.0264 mL	4.0528 mL	20.2641 mL
10 mM	0.2026 mL	1.0132 mL	2.0264 mL	10.1320 mL
20 mM	0.1013 mL	0.5066 mL	1.0132 mL	5.0660 mL
50 mM	0.0405 mL	0.2026 mL	0.4053 mL	2.0264 mL
100 mM	0.0203 mL	0.1013 mL	0.2026 mL	1.0132 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.

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Keywords

Topoisomerase ITopoisomeraseInhibitorinhibitHER2-targetingDxdCamptothecinsADCCytotoxinADC PayloadADC CytotoxinADC

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