Nelarabine

SKU: orb1223388

Description

Nelarabine is a purine nucleoside analog that is used as a cytotoxic agent in hematological malignancies. Nelarabine is converted into arabinosyl-guanine (ara-G) in the blood, and ara-G is selectively accumulated in T cells and malignant T-lymphoid cells, where it is phosphorylated to produce ara-GTP and incorporated into DNA.(In Vitro):Nelarabine (506U78) (0-20 μM; 48 h) induces cytotoxic effects in T-ALL cell lines.Nelarabine (5 or 2 μM; 48 h) promotes apoptosis in sensitive T-ALL cell lines and modulates PI3K/AKT/mTOR and MEK signaling.Nelarabine (10 μM; 0-48 h) resistance does not depend on expression of ENT1/2 transporters and is partly due to upregulation of PI3K, MEK, and Bcl2 signaling.(In Vivo):Nelarabine (506U78) (130 mg/kg/day; i.v.; 5 days) reduces leukemic burden and extends mouse survival in NSG mice xenografted with luciferase-expressing U937 cells.

Key Properties

• CAS Number: 121032-29-9
• MW: 297.27
• Purity: >98% (HPLC)
• Formula: C₁₁H₁₅N₅O₅
• SMILES: COC1=NC(N)=NC2=C1N=CN2[C@@H]1O[C@H](CO)[C@@H](O)[C@@H]1O
• Target: TLR
• Solubility: DMSO : 9.8 mg/mL. 32.97 mM

Bioactivity

• In Vivo:
  Nelarabine (506U78) (130 mg/kg/day; i. v. ; 5 days) reduces leukemic burden and extends mouse survival in NSG mice xenografted with luciferase-expressing U937 cells. Animal model: NSG mice xenografted with luciferase-expressing U937 cells. Dosage: 130 mg/kg/day. Administration: Intravenous injection, 5 days. Result: Reduced leukemic burden and extended mouse survival.
• In Vitro:
  Nelarabine (506U78) (0-20 μM; 48 h) induces cytotoxic effects in T-ALL cell lines. Nelarabine (5 or 2 μM; 48 h) promotes apoptosis in sensitive T-ALL cell lines and modulates PI3K/AKT/mTOR and MEK signaling. Nelarabine (10 μM; 0-48 h) resistance does not depend on expression of ENT1/2 transporters and is partly due to upregulation of PI3K, MEK, and Bcl2 signaling. Cell Viability Assay Cell line: T-ALL cell lines. Concentration: 0-20 μM. Incubation time: 48 h. Result: Cell viability decreased in a concentration-dependent fashion, and the IC50 values ranged between 2 and 5.5 μM for sensitive cell lines (MOLT-4, HSB-2, P12, DND41, JURKAT). Apoptosis Analysis Cell line: MOLT-4, JURKAT, P12-ICHIKAWA and DND41. Concentration: 5 μM (2 μM for MOLT-4 cells). Incubation time: 48 h. Result: Detected a marked increase in the percentage of early apoptotic and/or late apoptotic cells. Western blot analysis. Cell line: MOLT-4, JURKAT, P12-ICHIKAWA and DND41. Concentration: 5 μM (2 μM for MOLT-4 cells). Incubation time: 0, 6, 16, 24 and 48 h. Result: Documented a time-dependent cleavage of caspase 8, caspase 9, caspase 3, and poly(ADP-ribose) polymerase (PARP) in response to drug treatment.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Arranon, 506U78, GW506U78 | GW-506U78

Quick Database Links

Gene Symbol

TLR