Acelarin (NUC-1031)

For research use only.

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

Acelarin (NUC-1031) Chemical Structure

CAS No. 840506-29-8

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.

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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

Cell Research:

[1]

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  • 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.


    (Only for Reference)
Animal Research:

[1]

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

Solubility (25°C)

In vitro DMSO 100 mg/mL (172.27 mM)
Water Insoluble
Ethanol '20 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 580.47
Formula

C25H27F2N4O8P

CAS No. 840506-29-8
Storage powder
in solvent
Synonyms Fosgemcitabine palabenamide, 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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04163900 Recruiting 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

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

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

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DNA/RNA Synthesis Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID