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Clofarabine
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。
Clofarabine图片
CAS NO:123318-82-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
Clofarabine 是一种用于癌症研究的核苷类似物,通过与调节亚基上的变构位点结合,是一种有效的核糖核苷酸还原酶抑制剂 (IC50=65 nM) 。
Cas No.123318-82-1
别名氯法拉滨
化学名(2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol
Canonical SMILESC1=NC2=C(N1C3C(C(C(O3)CO)O)F)N=C(N=C2N)Cl
分子式C10H11ClFN5O3
分子量303.68
溶解度≥ 15.184mg/mL in DMSO
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Clofarabine is a DNA synthesis inhibitor and a substrate of Deoxycytidine kinase (dCK).
DCK is a key cytosolic enzyme in the DNA-synthesis salvage pathway and is responsible for the phosphorylation of clofarabine.
Clofarabine is phosphorylated to form clofarabine triphosphate, which competes with dATP for DNA polymerase-α and -ε. At the same time, clofarabine-monophosphate is incorporated into internal and terminal DNA sites, which impaired DNA elongation and repair. Clofarabine triphosphate inhibits ribonucleotide reductase with IC50 value of 65 nM, which then reduced dCTP and dATP. Clofarabine is efficiently transported into cells through nucleoside transporters hENT1, hENT2, and hCNT2. Clofarabine results in release of cytochrome c, apoptosis protease-activating factor 1 (APAF1), apoptotic-inducing factor (AIF) and caspase 9 into the cytosol. In both rapidly growing and quiescent tumours, clofarabine has anticancer activity because of its inhibition of DNA synthesis and induction of apoptosis.
Implanted human tumour xenografts in athymic nude or severe combined immune deficiency mice, Clofarabine administered intraperitoneally had significant antitumor activity.
References:
[1]. Bonate PL, Arthaud L, Cantrell WR Jr, et al. Discovery and development of clofarabine: a nucleoside analogue for treating cancer. Nat Rev Drug Discov, 2006, 5(10): 855-863.