Nelarabine (Arranon, 506U78) is a purine nucleoside analog converted to its corresponding arabinosylguanine nucleotide triphosphate (araGTP), resulting in inhibition of DNA synthesis and cytotoxicity. Nelarabine is well tolerated and has significant antitumor activity in T-cell acute lymphoblastic leukemia (T-ALL) and lymphoma (T-LBL). Nelarabine (506U78) has activity in T-cell malignancies, as evaluated in 2 Phase I and 5 Phase II studies. The mRNA levels of the transporters ENT1 and ENT2 were higher in Nelarabine-sensitive than -resistant samples.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 60 mg/mL|
In vitro efficacy of forodesine and nelarabine (ara-G) in pediatric leukemia.
Homminga I, et al. Blood. 2011 Aug 25;118(8):2184-90. PMID: 21730354.
Nelarabine for the treatment of patients with relapsed or refractory T-cell acute lymphoblastic leukemia or lymphoblastic lymphoma.
DeAngelo DJ. Hematol Oncol Clin North Am. 2009 Oct;23(5):1121-35, vii-viii. PMID: 19825456.
|Related DNA/RNA Synthesis Products|
Vidarabine is an antiviral drug by interfering with the synthesis of viral DNA, used to treat herpes simplex and varicella zoster viruses.
Uridine is a nucleoside, contains a uracil attached to a ribose ring via a β-N1-glycosidic bond.
Rifampin is a DNA-dependent RNA polymerase inhibitor, used to treat a number of bacterial infections.
Mitomycin C is an antineoplastic antibiotic by inhibiting DNA synthesis, used to treat different cancers.
Mercaptopurine is a widely used antileukemic agent and immunosuppressive drug that inhibits de novo purine synthesis through incorporation of thiopurine methyltransferase metabolites into DNA and RNA.
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