Acelarin (NUC-1031)

Catalog No.S9649 Batch:S964901

Technical Data

Formula	C₂₅H₂₇F₂N₄O₈P
Molecular Weight	580.47	CAS No.	840506-29-8
Solubility (25°C)*	In vitro	DMSO	100 mg/mL (172.27 mM)
		Ethanol	20 mg/mL (34.45 mM)
		Water	Insoluble
* <1 mg/ml means slightly soluble or insoluble. * 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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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

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]

In vivo

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

Protocol (from reference)

Cell Assay:^{^[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 Study:^{^[1]}	Animal Models MiaPaCa-2 bearing nude mice, BxPC-3 bearing nude mice Dosages 0.19 mM/kg, 0.076 mM/kg Administration IP

Cell Assay:^{^[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 Study:^{^[1]}

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

References

[1] Magdalena Slusarczyk, et al. J Med Chem. 2014 Feb 27;57(4):1531-42.

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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