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Acelarin

Name: Acelarin
Brand: TargetMol
SKU: T4060
Price: 38 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T4060Cas No. 840506-29-8

Alias NUC-1031

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

Acelarin

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Purity: 99.26%

Catalog No. T4060Alias NUC-1031Cas No. 840506-29-8

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

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$38	In Stock	In Stock
2 mg	$54	In Stock	In Stock
5 mg	$89	In Stock	In Stock
10 mg	$147	In Stock	In Stock
25 mg	$288	In Stock	In Stock
50 mg	$442	In Stock	In Stock
100 mg	$617	In Stock	In Stock
200 mg	$873	In Stock	-
1 mL x 10 mM (in DMSO)	$98	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.26%

Appearance:Solid

Color:White

Resource Download

COA LCMS HNMR

Product Introduction

Acelarin AI Summary

Acelarin exhibits both cytostatic and cytotoxic activities against a broad range of cell lines, including mouse L1210, human CEM, MIAPaCa2, BxPC3, RT112, PANC1, African green monkey Vero, and human HEL cells. It shows prodrug activation in human and dog serum and maintains a metabolic stability in human liver microsomes. Notably, it has a half-life of 8.3 hours and achieves a maximum concentration of 475,000 nM in humans. The compound demonstrates toxicity levels causing various adverse effects such as anemia, fatigue, transaminitis, and thrombocytopenia in patients with solid malignancies, and body weight loss in Balb/c nude mice xenografted with human MIAPaCa2 cells. Additionally, Acelarin shows significant antiviral activity against SARS-CoV-2, Human cytomegalovirus, and Varicella zoster virus by inhibiting virus plaque formation. In terms of cytotoxic potency, it exhibits the highest activity against MIA PaCa-2 cells with an LC50 of 100.0 nM, and moderate activity against KG-1a, HT-29, and BXPC-3 cells with LC50 values of 280.0 nM, 1300.0 nM, and 2290.0 nM, respectively. It also displays good stability in cryopreserved human hepatocytes. The antiproliferative efficacy is evidenced by IC50 values ranging from 31.1 nM to 350.3 nM across different human cancer cell lines and the induction of apoptosis in BXPC-3 cells. In in vivo studies, Acelarin shows significant antitumor activity, with a tumor growth inhibition (TGI) of 55.61% and a relative increment ratio (T/C) of 51.9% in 22Rv1 cells xenografted in castrated male nude Balb/c mice when administered at 50 mg/kg biweekly for 28 days..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Acelarin (NUC-1031) (NUC-1031) is a ProTide enhancement and transformation of the nucleoside analog, gemcitabine.
Targets&IC50	DNA synthesis:EC50 : 0.2 nM
Synonyms	NUC-1031

Chemical Properties

Molecular Weight	580.47
Formula	C₂₅H₂₇F₂N₄O₈P
Cas No.	840506-29-8
Smiles	FC1(F)[C@@H](O[C@H](COP(OC2=CC=CC=C2)(N[C@H](C(OCC3=CC=CC=C3)=O)C)=O)[C@H]1O)N4C(=O)N=C(N)C=C4
Relative Density.	1.51 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 55 mg/mL (94.75 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.45 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.7227 mL	8.6137 mL	17.2274 mL	86.1371 mL
5 mM	0.3445 mL	1.7227 mL	3.4455 mL	17.2274 mL
10 mM	0.1723 mL	0.8614 mL	1.7227 mL	8.6137 mL
20 mM	0.0861 mL	0.4307 mL	0.8614 mL	4.3069 mL
50 mM	0.0345 mL	0.1723 mL	0.3445 mL	1.7227 mL

Calculator

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc