Nelarabine

Catalog No.S1213 Synonyms: 506U78

For research use only.

Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.

Nelarabine  Chemical Structure

CAS No. 121032-29-9

Selleck's Nelarabine has been cited by 10 Publications

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Biological Activity

Description Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
Features Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.
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]

Protocol (from reference)

Cell Research: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 Research:[4]
  • Animal Models: Healthy adult male rhesus monkeys
  • Dosages: 35 mg/kg
  • Administration: Administered via i.v.

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
saline
For best results, use promptly after mixing.

3mg/mL

Chemical Information

Molecular Weight 297.27
Formula

C11H15N5O5

CAS No. 121032-29-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles COC1=NC(=NC2=C1N=CN2C3C(C(C(O3)CO)O)O)N

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02619630 Recruiting Drug: nelarabine T-cell Adult Acute Lymphoblastic Leukemia Assistance Publique - Hôpitaux de Paris December 2015 Phase 2
NCT01094860 Completed Drug: Nelarabine Leukemia M.D. Anderson Cancer Center|GlaxoSmithKline June 8 2010 Phase 1
NCT01376115 Completed Drug: Nelarabine Cancer Novartis Pharmaceuticals|Novartis January 18 2008 --

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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

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