1. Cell Cycle/DNA Damage
  2. DNA/RNA Synthesis
  3. Acelarin

Acelarin (Synonyms: NUC-1031)

Cat. No.: HY-100885 Purity: 99.76%
Handling Instructions

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

For research use only. We do not sell to patients.

Acelarin Chemical Structure

Acelarin Chemical Structure

CAS No. : 840506-29-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 506 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Acelarin (NUC-1031) is a ProTide transformation and enhancement of the widely-used nucleoside analogue, gemcitabine.

IC50 & Target

EC50:0.2 nM (DNA synthesis inhibitor)[1]

In Vitro

Gemcitabine is a nucleoside analogue commonly used in cancer therapy but with limited efficacy due to a high susceptibility to cancer cell resistance. The addition of a phosphoramidate motif to the gemcitabine can protect it against many of the key cancer resistance mechanisms. A series of gemcitabine phosphoramidate prodrugs are synthesized and screened for cytostatic activity in a range of different tumor cell lines. Among the synthesized compounds, NUC-1031 is shown to be potent in vitro.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

The ProTide demonstrates a significant reduction in tumor size against pancreatic xenograft models compared with the gemcitabine treated group, and less adverse effects on body weight, indicating a better safety profile. Data strongly suggests that the ProTides are not reliant on kinases or nucleoside transporters to exert their activity inside tumor cells and remain stable in the presence of deaminases. The ProTide NUC-1031 is currently advancing through phase I/II clinical studies and has already generated strong pharmacokinetic data that confirm significantly higher intracellular levels of gemcitabine triphosphate, together with promising early efficacy signals and a favorable safety profile. The phosphoramidate chemistry is potentially a great source of new and very effective anticancer agents, bringing a considerable array of advanced treatments specifically designed to overcome cancer resistance mechanisms that will benefit a greater proportion of patients[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

580.47

Formula

C₂₅H₂₇F₂N₄O₈P

CAS No.

840506-29-8

SMILES

O=C1N=C(N)C=CN1[[email protected]@H]2O[[email protected]](COP(OC3=CC=CC=C3)(N[[email protected]](C(OCC4=CC=CC=C4)=O)C)=O)[[email protected]@H](O)C2(F)F

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 36 mg/mL (62.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7227 mL 8.6137 mL 17.2274 mL
5 mM 0.3445 mL 1.7227 mL 3.4455 mL
10 mM 0.1723 mL 0.8614 mL 1.7227 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

NUC-1031(5.0 mg) is dissolved in DMSO (0.050 mL) and D2O (0.15 mL). After recording the control 31P NMR at 37 °C, a previously defrosted human, rat, or dog serum (0.30 mL) is added to the sample, which is next submitted to the 31P NMR experiments at 37°C. The spectra are recorded every 30 min over 13 h. 31P NMR recorded data are processed and analyzed with the Bruker Topspin 2.1 program[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

Balb/c nude mice are female, six to eight week old, with the weight of 20 ± 2 g. They are intraperitoneally given NUC-1031 (i.p 0.228 mmol/kg, 132.3 mg/kg, 2×/WK) or vehicle for 2 weeks. NUC-1031 is dissolved in 40% Captisol solution. (40% Captisol is prepared by dissolving 20mg of Captisol with pure water, and made the final volume 50 mL. The solvent is filtered with 0.22 μm filter). Mice are monitored daily for body weight change and clinical symptoms for 2 weeks[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.76%

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Keywords:

AcelarinNUC-1031NUC1031NUC 1031DNA/RNA SynthesisInhibitorinhibitorinhibit

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