Nelarabine

Catalog No.S1213 Batch:S121303

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Technical Data

Formula

C11H15N5O5
Molecular Weight 297.27 CAS No. 121032-29-9
Solubility (25°C)* In vitro DMSO 60 mg/mL (201.83 mM)
Water 5 mg/mL (16.81 mM)
Ethanol 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.)

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Biological Activity

Description Nelarabine (506U78,Arranon) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Targets
DNA synthesis (PER-255 cells) [1] DNA synthesis (HSB2 cells) [1] DNA synthesis (ALL-SIL cells) [1] DNA synthesis (JURKAT cells) [1]
67 nM 0.44 μM 1.24 μM 2.15 μM
In vitro The IC50 of Nelarabine is 25-fold and 113-fold higher than ARAC in T- and B-lineage, respectively. T-ALL cells are eightfold more sensitive to Nelarabine than B-lineage but there is considerable overlap. The efficacy of NEL in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively. [1] Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. [2]Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity. [3]
In vivo The Nelarabine plasma AUC is 2.82 mM minutes and the ara-G plasma AUC is 20 mM minutes. The terminal half-life of Nelarabine in plasma is 25 min, clearance is 42 mL/minutes/kg, and central volume of distribution is 1.1 L/kg. The terminal half-life of ara-G in plasma is 182 minutes and the central volume of distribution is 1.4 L/kg. In CSF the terminal half-life of Nelarabine is 77 minutes and of ara-G is 232 minutes. The AUCcsf:AUCplasma is 29 % for Nelarabine and 23 % for ara-G. Nelarabine and ara-G do not accumulate with daily infusions because of their relatively short half-lives. [4]
Features Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.

Protocol (from reference)

Cell Assay:sup>[1]
  • Cell lines

    HSB2, ALL-SIL, JURKAT and PER-255 cell lines

  • Concentrations

    0.125 μg/mL - 8 μg/mL

  • Incubation Time

    96 hours

  • Method

    HSB2, ALL-SIL, JURKAT and PER-255 cell lines are tested for drug resistance using the MTT assay. Nelarabine are incubated over 4 days, with concentration tested in triplicate. The IC50 (drug concentration that inhibits cell growth by 50%) is used as the measure of drug resistance. Data represent the average of 2-6 experiments performed on separate occasions. In cases where 50% cytotoxicity is not achieved by even the highest dose in a particular experiment, the IC50 is recorded as double the highest concentration tested.
Animal Study:[4]
  • Animal Models

    Healthy adult male rhesus monkeys

  • Dosages

    35 mg/kg

  • Administration

    Administered via i.v.

Customer Product Validation

Data from [Data independently produced by , , J Hematol Oncol, 2016, 9(1):114.]

Selleck's Nelarabine has been cited by 13 publications

Targeting Ribonucleotide Reductase Induces Synthetic Lethality in PP2A-Deficient Uterine Serous Carcinoma [ Cancer Res, 2022, 82(4):721-733] PubMed: 34921012
Drug screen in iPSC-Neurons identifies nucleoside analogs as inhibitors of (G4C2)n expression in C9orf72 ALS/FTD [ Cell Rep, 2022, 39(10):110913] PubMed: 35675776
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] PubMed: 35207746
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] PubMed: 35118583
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] PubMed: 34731453
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] PubMed: 34304386
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] PubMed: 34383271
Prevention of SARS-CoV-2 Proliferation with a Novel and Potent Main Protease Inhibitor by Docking, ADMET, MM-PBSA, and Molecular Dynamics Simulation [ World Scientific, 2021, Vol. 20, No. 03, pp. 305-322] PubMed: None
Overcoming Wnt-β-catenin Dependent Anticancer Therapy Resistance in Leukaemia Stem Cells [ Nat Cell Biol, 2020, 20] PubMed: 32313104
Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58] PubMed: 32099531

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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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