Nelarabine

製品コードS1213 バッチS121304

印刷

化学情報

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

3 mg/mL (10.09 mM)

Ethanol

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	saline この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.000mg/ml (10.09mM)	Taking the 1 mL working solution as an example, add 3 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

* <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) はプリンヌクレオシド類似体であり、腫瘍細胞におけるIC50が0.067～2.15 µMのDNA合成阻害剤です。
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 this compound than B-lineage but there is considerable overlap. The efficacy of this chemical in T-lineage and B-lineage cell lines is 25-fold and 113-fold less than ARAC, respectively. It acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. This agent demonstrated significant antineoplastic activity with acceptable toxicity.
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 this compound 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 this chemical is 77 minutes and of ara-G is 232 minutes. The AUCcsf:AUCplasma is 29 % for this agent and 23 % for ara-G. This compound and ara-G do not accumulate with daily infusions because of their relatively short half-lives.
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.

参考

https://pubmed.ncbi.nlm.nih.gov/17391490/
https://pubmed.ncbi.nlm.nih.gov/16925505/
https://pubmed.ncbi.nlm.nih.gov/17344466/

https://pubmed.ncbi.nlm.nih.gov/16953392/

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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.]

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長期の保管のために-20°Cの下で製品を保ってください。

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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