Home DNA Damage/DNA Repair DNA/RNA Synthesis inhibitor Nelarabine For research use only.

Nelarabine

Synonyms: 506U78,Arranon

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

Nelarabine Chemical Structure

Nelarabine Chemical Structure

CAS No. 121032-29-9

Purity & Quality Control

Nelarabine Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

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.
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
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]
Cell Research 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.
In Vivo
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]
Animal Research Animal Models Healthy adult male rhesus monkeys
Dosages 35 mg/kg
Administration Administered via i.v.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02619630 Recruiting
T-cell Adult Acute Lymphoblastic Leukemia
Assistance Publique - Hôpitaux de Paris
 December 2015 Phase 2
NCT01094860 Completed
Leukemia
M.D. Anderson Cancer Center|GlaxoSmithKline
 June 8 2010 Phase 1
NCT01376115 Completed
Cancer
Novartis Pharmaceuticals|Novartis
 January 18 2008 --

Chemical Information & Solubility

Molecular Weight 297.27 Formula

C11H15N5O5
CAS No. 121032-29-9 SDF Download Nelarabine SDF
Smiles COC1=NC(=NC2=C1N=CN2C3C(C(C(O3)CO)O)O)N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (201.83 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble


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