Nelarabine cas 121032-29-9

Nelarabine (Arranon, 506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells. Nelarabine is a chemotherapy drug used in T-cell acute lymphoblastic leukemia. IC50 Value: 0.44 uM (HSB2 cell lines); 1.24 μM(ALL-SIL cell lines); 2.15 μM(JURKAT cell lines); 0.067 uM (PER-255 cell lines) [1] Target: Nucleoside antimetabolite/analog 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]. in vivo: The median age was 34 years (range, 16-66 years); 32 (82%) patients were male. The rate of complete remission was 31% (95% confidence interval [CI], 17%, 48%) and the overall response rate was 41% (95% CI, 26%, 58%). The principal toxicity was grade 3 or 4 neutropenia and thrombocytopenia, occurring in 37% and 26% of patients, respectively. Nelarabine has activity in T-cell malignancies, as evaluated in 2 Phase I and 5 Phase II studies. It received accelerated approval from the FDA based on the resuits of 2 Phase II trials, one in pediatric patients (PGAA 2001) and the other in adults (CALGB 19801) Toxicity: The principal toxicity was grade 3 or 4 neutropenia and thrombocytopenia, occurring in 37% and 26% of patients, respectively. Clinical trial: Drug Use Investigation for Arranon G (Nelarabine) Injection 250 mg.

Properties:

Appearance & Physical State: White solid

Density: 1.98 g/cm3

Boiling Point: 721ºC at 760 mmHg

Melting Point: 209-217ºC

Flash Point: 389.9ºC

Refractive Index: 1.829

Vapor Pressure 8.06E-22mmHg at 25°C

Related Prodcuts:

Cisplatin; Gemcitabine HCL; Bleomycin Sulfate; Temozolomide; Carmustine; CX-5461; Fludarabine Phosphate; Cladribine; Trifluridine; Daptomycin; Vorinostat

[1] Beesley AH, et al. Br J Haematol. 2007, 137(2), 109-116.

[2] Kline J, et al. Expert Opin Pharmacother. 2006, 7(13), 1791-1799.

[3] DeAngelo DJ, et al. Blood. 2007, 109(12), 5136-5142.