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Deruxtecan Topoisomerase I Inhibitor

Name: Deruxtecan
Brand: Selleck Chemicals
SKU: S9795
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9795

Deruxtecan is an ADC drug-linker conjugate composed of the cleavable glycine–glycine–phenylalanine–glycine tetrapeptide-based linker, a self-immolative amino methylene spacer, and a novel topoisomerase 1 inhibitor payload that is a derivative of exatecan (DX-8951).

Chemical Structure

Molecular Weight: 1034.05

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Quality Control

Batch: S979501 DMSO]100 mg/mL]false]]]false]]]false Purity: 99.86%

Cited in Nature Medicine for its top-tier quality
COA
SDS
Datasheet

99.86

Related Targets	Bcl-2 Caspase K-Ras PD-1/PD-L1 Ferroptosis p53 Apoptosis related Synthetic Lethality STAT TNF-alpha
Other ADC Linker Products	DSS Crosslinker MC-VC-PAB-PNP MC-Val-Cit-PAB Fmoc-Val-Ala-PAB Boc-Val-Cit-PAB-PNP Sulfo-SMCC sodium Succinic anhydride Fmoc-Val-Cit-PAB DSP Crosslinker PDEC-NB

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (96.7 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	5.000mg/ml (4.84mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.830mg/ml (0.80mM)	Taking the 1 mL working solution as an example, add 50 μL of 16.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	1034.05	Formula	C₅₂H₅₆FN₉O₁₃	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	1599440-13-7	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent

Mechanism of Action

References	[1] https://pubmed.ncbi.nlm.nih.gov/32067685/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06350097	Not yet recruiting	Non-small Cell Lung Cancer	AstraZeneca\|Daiichi Sankyo	May 16 2024	Phase 3
NCT06222489	Not yet recruiting	Non-Small Cell Lung Carcinoma\|Advanced Non-Small Cell Squamous Lung Cancer\|EGFR Gene Mutation	The Netherlands Cancer Institute\|Daiichi Sankyo	May 1 2024	Phase 2
NCT05620914	Not yet recruiting	Brain Metastases Adult	Mustafa Khasraw MBChB MD FRCP FRACP\|Daiichi Sankyo\|Duke University	April 2024	Early Phase 1
NCT06331169	Not yet recruiting	Breast Cancer	Fudan University	April 1 2024	Phase 1
NCT05458674	Recruiting	Breast Cancer	Criterium Inc.	January 1 2024	Phase 2
NCT05480384	Recruiting	Esophageal Adenocarcinoma\|Esophageal Cancer\|HER-2 Protein Overexpression\|Gastroesophageal-junction Cancer	Brown University\|AstraZeneca	July 14 2023	Phase 2

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

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