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Nelarabine(Arranon 506U78)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Nelarabine(Arranon 506U78)图片
CAS NO:121032-29-9
规格:≥98%
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议
250mg电议
500mg电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)297.27
FormulaC11H15N5O5
CAS No.121032-29-9
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 60 mg/mL (201.8 mM)
Water: 3 mg/mL (10.1 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL
SynonymsGW 506U78; 506 U 78; NSC-686673; 506 U78; GW-506U78; NS-686673; 506U78, GW506U78; Arranon; NSC686673;
实验参考方法
In Vitro

In vitro activity: 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. Nelarabine acts by inhibiting DNA synthesis and inducing apoptosis in susceptible cells. Nelarabine demonstrated significant antineoplastic activity with acceptable toxicity.


Cell Assay: 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.

In VivoThe 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.
Animal modelHealthy adult male rhesus monkeys
Formulation & Dosage35 mg/kg; i.v. injection
References

Br J Haematol. 2007 Apr;137(2):109-16; Expert Opin Pharmacother. 2006 Sep;7(13):1791-9; Cancer Chemother Pharmacol. 2007 May;59(6):743-7.