Acelarin (NUC-1031)

Catalog No.S9649 Synonyms: Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389

For research use only.

Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.

Acelarin (NUC-1031) Chemical Structure

CAS No. 840506-29-8

Purity & Quality Control

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Biological Activity

Description Acelarin (NUC-1031, Fosgemcitabine palabenamide, CPF-31, MTL-007, GTPL7389), a prodrug based on an aryloxy phosphoramidate derivative of gemcitabine, is a DNA synthesis inhibitor with EC50 of 0.2 nM.
Targets
DNA synthesis [1]
(Cell-free assay)
0.2 nM(EC50)
In vitro

NUC-1031 is a gemcitabine phosphoramidate prodrug with potent cytostatic activity in a range of different tumor cell lines. Importantly, compared with gemcitabine, NUC-1031 activation is significantly less dependent on deoxycytidine kinase and on nucleoside transporters, and it is resistant to cytidine deaminase-mediated degradation.[1]

In vivo

NUC-1031 shows a significant reduction in tumor volumes in vivo in pancreatic cancer xenografts.[1]

Protocol (from reference)

Cell Research:

[1]

  • 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.

Animal Research:

[1]

  • Animal Models: MiaPaCa-2 bearing nude mice, BxPC-3 bearing nude mice
  • Dosages: 0.19 mM/kg, 0.076 mM/kg
  • Administration: IP

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 580.47
Formula

C25H27F2N4O8P

CAS No. 840506-29-8
Storage 3 years -20°C powder
2 years -80°C in solvent
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

In vivo Formulation Calculator (Clear solution)

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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
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04163900 Terminated Drug: NUC-1031|Drug: Gemcitabine|Drug: Cisplatin Biliary Tract Cancer NuCana plc December 24 2019 Phase 3
NCT02351765 Completed Drug: Acelarin|Drug: Cisplatin Biliary Tract Cancer|Gallbladder Cancer|Cholangiocarcinoma|Ampullary Cancer The Christie NHS Foundation Trust January 2016 Phase 1
NCT02303912 Completed Drug: Nuc-1031 and Carboplatin Recurrent Ovarian Cancer Imperial College Healthcare NHS Trust November 2014 Phase 1
NCT01621854 Completed Drug: NUC-1031 Cancer Imperial College London|Nucana October 2012 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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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