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Dxd

Name: Dxd
Brand: TargetMol
SKU: T11249L
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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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

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Purity: 99.85%

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 Size	Price	USA Warehouse	Global Warehouse
1 mg	$39	In Stock	In Stock
5 mg	$68	In Stock	In Stock
10 mg	$97	In Stock	In Stock
25 mg	$159	In Stock	In Stock
50 mg	$233	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$74	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

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Purity:99.85%

Appearance:Solid

Color:White to Yellow

Resource Download

COA HNMR HPLC

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	SKBR3 cells:6.7 ng/mL, Topo I:0.31 μM, MDA-MB-468 cells:> 10,000 ng/mL, KPL-4 cells:26.8 ng/mL, NCI-N87 cells:25.4 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	493.48
Formula	C₂₆H₂₄FN₃O₆
Cas No.	1599440-33-1
Smiles	CC[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

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: insoluble

DMSO: 51.5 mg/mL (104.36 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.0264 mL	10.1321 mL	20.2642 mL	101.3212 mL
5 mM	0.4053 mL	2.0264 mL	4.0528 mL	20.2642 mL
10 mM	0.2026 mL	1.0132 mL	2.0264 mL	10.1321 mL
20 mM	0.1013 mL	0.5066 mL	1.0132 mL	5.0661 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

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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, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

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 TargetMol | reagent 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 TargetMol | reagent 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 TargetMol | reagent 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

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc