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: 121032-29-9

Selleck's Nelarabine has been cited by 13 Publications

1 Customer Review

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Nelarabine Related Products

Signaling Pathway

DNA/RNA Synthesis Signaling Pathways

DNA/RNA Synthesis Signaling Pathway

Choose Selective DNA/RNA Synthesis Inhibitors

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


Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

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

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Nelarabine | Nelarabine supplier | purchase Nelarabine | Nelarabine cost | Nelarabine manufacturer | order Nelarabine | Nelarabine distributor