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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.
| Molecular Weight | 297.27 |
| Formula | C11H15N5O5 |
| CAS Number | 121032-29-9 |
| Solubility (25°C) | DMSO ≥ 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related DNA/RNA Synthesis Products |
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| Clofarabine
Clofarabine inhibits the enzymatic activities of ribonucleotide reductase (IC50 = 65 nM) and DNA polymerase. |
| Gemcitabine Hydrochloride
Gemcitabine (Gemzar, LY188011) inhibits DNA synthesis with an IC50 of 0.06 µM. |
| Mizoribine
Mizoribine (Bredinin) is an imidazole nucleoside and an immunosuppressive agent with an IC50 of approximately 100 μM. Mizoribine inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively. |
| Capecitabine
Capecitabine is an orally-administered chemotherapeutic agent. Capecitabine is a precursor, that is enzymatically converted to 5-fluorouracil in the tumor, where it inhibits DNA synthesis and slows growth of tumor tissue. Capecitabine may inhibit cytochrome CYP2C9 enzyme, and therefore increase levels of substrates such as phenytoin and other substrates of CYP2C9. |
| Temozolomide
Temozolomide (TMZ) is an oral DNA methylating, chemotherapeutic agent. |
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