Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Acelarin (NUC-1031) For research use only.

Acelarin (NUC-1031)

Synonyms: CPF-31, MTL-007, GTPL7389

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

Acelarin (NUC-1031) Chemical Structure

Acelarin (NUC-1031) Chemical Structure

CAS: 840506-29-8

Purity & 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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Biological Activity

Description Acelarin (NUC-1031, CPF-31, MTL-007, GTPL7389) is a DNA synthesis inhibitor with EC50 of 0.2 nM.
Targets
DNA synthesis [1]
(Cell-free assay)
0.2 nM(EC50)
In vitro
In vitro

NUC-1031 is a prodrug with potent cytostatic activity in a range of different tumor cell lines. Importantly, NUC-1031 activation is significantly less dependent on deoxycytidine kinase and on nucleoside transporters, and it is resistant to cytidine deaminase-mediated degradation.[1]
Cell Research Cell lines Murine leukemia L1210, human lymphocyte CEM
Concentrations 1 μM
Incubation Time 1 h
Method

Metabolic Stability (Cryopreserved Hepatocytes, Human) Assay. The assay is contracted and performed by Cerep according to the published procedure.Pooled cryopreserved hepatocytes are thawed, washed, and resuspended in Krebs-Heinslet buffer (pH 7.3). The reaction is initiated by adding Acelarin (NUC-1031) (1 μM final concentration) into cell suspension and incubated in a final volume of 100 μL on a flatbottom 96-well plate for 0 and 60 min, respectively, at 37 ℃/5% CO2. The reaction is stopped by adding 100 μL of acetonitrile into the incubation mixture. Samples are then mixed gently and briefly on a plate shaker, transferred completely to a 0.8 mL V-bottom 96-well plate, and centrifuged at 2550 × g for 15 min at room temperature. Each supernatant (150 μL) is transferred to a clean cluster tube, followed by HPLC-MS/MS analysis on a Thermo Electron triplequadrupole system.
In Vivo
In vivo

NUC-1031 shows a significant reduction in tumor volumes in vivo in pancreatic cancer xenografts.[1]
Animal Research Animal Models MiaPaCa-2 bearing nude mice, BxPC-3 bearing nude mice
Dosages 0.19 mM/kg, 0.076 mM/kg
Administration IP
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

Chemical lnformation & Solubility

Molecular Weight 580.47 Formula

C25H27F2N4O8P
CAS No. 840506-29-8 SDF --
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
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (172.27 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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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.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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