research use only

Nelarabine DNA/RNA Synthesis inhibitor

Cat.No.S1213

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

Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (201.83 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 3 mg/mL

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight
Dilution Calculator Molecular Weight Calculator

In vivo
Batch:

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.

Chemical Information, Storage & Stability

Molecular Weight 297.27 Formula

C11H15N5O5

Storage (From the date of receipt)
CAS No. 121032-29-9 Download SDF Storage of Stock Solutions

Synonyms 506U78,Arranon SMILES COC1=NC(=NC2=C1N=CN2C3C(C(C(O3)CO)O)O)N

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Features
Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.
Targets/IC50/Ki
DNA synthesis (PER-255 cells)
67 nM
DNA synthesis (HSB2 cells)
0.44 μM
DNA synthesis (ALL-SIL cells)
1.24 μM
DNA synthesis (JURKAT cells)
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 this compound than B-lineage but there is considerable overlap. The efficacy of this chemical in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively. It acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. This agent demonstrated significant antineoplastic activity with acceptable toxicity.
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 this compound 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 this chemical is 77 minutes and of ara-G is 232 minutes. The AUCcsf:AUCplasma is 29 % for this agent and 23 % for ara-G. This compound and ara-G do not accumulate with daily infusions because of their relatively short half-lives.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/16953392/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-07-30)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07072585 NOT_YET_RECRUITING
Stage II T Lymphoblastic Leukemia/Lymphoma; Stage III T Lymphoblastic Leukemia/Lymphoma; Stage IV T Lymphoblastic Leukemia/Lymphoma; T Acute Lymphoblastic Leukemia; T Lymphoblastic Lymphoma
Children's Oncology Group
2026-08-28 PHASE2; PHASE3
NCT07294677 RECRUITING
Leukemia; Lymphoma
University of Chicago
2026-03-17 PHASE1; PHASE2
NCT06390319 RECRUITING
T-cell Acute Lymphoblastic Leukemia; T-cell Lymphoma; Mixed Phenotype Acute Leukemia
St. Jude Children's Research Hospital
2024-12-27 PHASE2
NCT03020030 ACTIVE_NOT_RECRUITING
Acute Lymphoblastic Leukemia, Pediatric
Dana-Farber Cancer Institute
2017-03-03 PHASE3
NCT00501826 RECRUITING
T Acute Lymphoblastic Leukemia; T Lymphoblastic Lymphoma
M.D. Anderson Cancer Center
2007-07-11 PHASE2
NCT03117751 ACTIVE_NOT_RECRUITING
Acute Lymphoblastic Leukemia; Acute Lymphoblastic Lymphoma
St. Jude Children's Research Hospital
2017-03-29 PHASE2; PHASE3

Read more about Clinical Trials

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Signaling Pathway Map