Nelarabine

製品コードS1213 バッチS121303

印刷

化学情報

Chemical Structure Synonyms 506U78,Arranon Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C11H15N5O5
分子量 297.27 CAS No. 121032-29-9
Solubility (25°C)* 体外 DMSO 60 mg/mL (201.83 mM)
Water 5 mg/mL (16.81 mM)
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Nelarabine (506U78) is a purine nucleoside analog and DNA synthesis inhibitor with IC50 from 0.067-2.15 μM in tumor cells.
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] Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. [2]Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity. [3]
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. [4]
特徴 Nelarabine is rapidly converted into ara-G through demethoxylation by adenosine deaminase.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 HSB2, ALL-SIL, JURKAT and PER-255 cell lines
濃度 0.125 μg/mL - 8 μg/mL
反応時間 96 hours
実験の流れ 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.
動物実験 動物モデル Healthy adult male rhesus monkeys
投薬量 35 mg/kg
投与方法 Administered via i.v.

カスタマーフィードバック

Data from [Data independently produced by , , J Hematol Oncol, 2016, 9(1):114.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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人間や獣医の診断であるか治療的な使用のためにでない。

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