123318-82-1Clofarabine

产品属性：

Cas No.123318-82-1

别名

化学名 (2R,3R,4S,5R)-5-(6-amino-2-chloropurin-9-yl)-4-fluoro-2-(hydroxymethyl)oxolan-3-ol

分子式 C10H11ClFN5O3

分子量 303.68

溶解度 ≥ 15.184mg/mL in DMSO

储存条件 Store at -20°C
General tips  For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition     Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
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.