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Acelarin (NUC-1031) DNA/RNA Synthesis inhibitor

Name: Acelarin (NUC-1031)
Brand: Selleck Chemicals
SKU: S9649
Availability: InStock
Rating: 5 (1 reviews)

Cat.No.S9649

Acelarin (NUC-1031, CPF-31, MTL-007, GTPL7389) is a DNA synthesis inhibitor with EC50 of 0.2 nM.

Chemical Structure

Molecular Weight: 580.47

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S964901 DMSO]100 mg/mL]false]Ethanol]20 mg/mL]false]Water]Insoluble]false Purity: 99.84%

99.84

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Chemical Information, Storage & Stability

Molecular Weight	580.47	Formula	C₂₅H₂₇F₂N₄O₈P	Storage (From the date of receipt)	3 years -20°C powder
CAS No.	840506-29-8	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CPF-31, MTL-007, GTPL7389			Smiles	CC(C(=O)OCC1=CC=CC=C1)NP(=O)(OCC2C(C(C(O2)N3C=CC(=NC3=O)N)(F)F)O)OC4=CC=CC=C4

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (172.27 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

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.	5mg/ml (8.61mM)	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.	0.167mg/ml (0.29mM)	Taking the 1 mL working solution as an example, add 50 μL of 3.34 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.

Mechanism of Action

Targets/IC₅₀/Ki	DNA synthesis ^[1] (Cell-free assay) 0.2 nM(EC50)
In vitro	Acelarin (NUC-1031) is a prodrug with potent cytostatic activity in a range of different tumor cell lines. Importantly, its activation is significantly less dependent on deoxycytidine kinase and on nucleoside transporters, and it is resistant to cytidine deaminase-mediated degradation.^[1]
In vivo	In pancreatic cancer xenografts, Acelarin (NUC-1031) shows a significant reduction in tumor volumes in vivo.^[1]
References	[1] https://pubmed.ncbi.nlm.nih.gov/24471998/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT02351765	Completed	Biliary Tract Cancer\|Gallbladder Cancer\|Cholangiocarcinoma\|Ampullary Cancer	The Christie NHS Foundation Trust	January 2016	Phase 1
NCT02303912	Completed	Recurrent Ovarian Cancer	Imperial College Healthcare NHS Trust	November 2014	Phase 1
NCT01621854	Completed	Cancer	Imperial College London\|Nucana	October 2012	Phase 1

Tech Support

Handling Instructions

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