Nelarabine

SKU: orb1300623

Description

Nelarabine (GW 506U78) is a purine nucleoside analog that inhibits DNA synthesis, demonstrating potent antitumor activity with IC50 values ranging from 0.067 to 2.15 μM in cellular assays. It is widely used in research for studying T-cell acute lymphoblastic leukemia (T-ALL) and has been evaluated in both in vitro and in vivo experimental models.

Research Area

Cell Biology, Molecular Biology

Key Properties

• CAS Number: 121032-29-9
• MW: 297.27
• Purity: 99.60% (May vary between batches)
• Formula: C₁₁H₁₅N₅O₅
• SMILES: COc1nc(N)nc2n(cnc12)[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1O
• Target: Nucleoside Antimetabolite/Analog,DNA/RNA Synthesis,Apoptosis
• Solubility: H2O:3 mg/mL (10.09 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:1 mg/mL (3.36 mM);DMSO:5 mg/mL (16.82 mM)

Bioactivity

• Target IC50:
  DNA synthesis (PER-255 cells):0.067-2.15 μM
• 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.
• 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. Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity.
• Cell Research:
  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.(Only for Reference)

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

GW 506U78, HSB-2, MOLT-4, Nelzarabine, Nelarabine, P12, NucleosideAntimetabolite, Nucleoside Antimetabolite/Analog, Nucleoside Antimetabolite, JURKAT, inhibit, Inhibitor, DND41, DNASynthesis, DNA Synthesis, DNA synthesis (ALL-SIL cells), DNA synthesis (HSB2 cells), DNA synthesis (JURKAT cells), DNA synthesis (PER-255 cells), 506U78, acute lymphoblastic leukaemia, Analog, Apoptosis, T-ALL, RNASynthesis, RNA Synthesis

Compound Identifiers

PubChem CID

3011155