Cytarabine hydrochloride 是一种核苷类似物,可导致 S 期细胞周期停滞并抑制DNA聚合酶。Cytarabine 抑制DNA 合成,IC50为 16 nM。Cytarabine hydrochloride对HSV具有抗病毒作用。
产品描述
Cytarabine hydrochloride is a nucleoside analog that causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC 50 of 16 nM. Cytarabine hydrochloride has antiviral effects against HSV.
体外活性
Cytarabine is phosphorylated into a triphosphate form (Ara-CTP) involving deoxycytidine kinase (dCK), which competes with dCTP for incorporation into DNA, and then blocks DNA synthesis by inhibiting the function of DNA and RNA polymerases. Cytarabine displays a higher growth inhibitory activity towards wild-type CCRF-CEM cells with IC 50 of 16 nM compared to other acute myelogenous leukemia (AML) cells [1]. Cytarabine apparently induces apoptosis of rat sympathetic neurons at 10 μM, of which 100 μM shows the highest toxicity and kills over 80% of the neurons by 84 hours, involving the release of mitochondrial cytochrome-c and the activation of caspase-3, and the toxicity can be attenuated by p53 knockdown and delayed by bax deletion [2].
体内活性
Cytarabine (250 mg/kg) also leads to placental growth retardation and increases placental trophoblastic cells apoptosis in the placental labyrinth zone of the pregnant Slc:Wistar rats, which increases from 3 hour after the treatment and peaks at 6 hour before returning to control levels at 48 hour, with remarkably enhanced p53 protein, p53 trancriptional target genes such as p21, cyclinG1 and fas and caspase-3 activity [3]. Cytarabine is highly effective against acute leukaemias, which causes the chCytarabineteristic G1/S blockage and synchronization, and increases the survival time for leukaemic Brown Norway rats in a weak dose-related fashion indicating that the use of higher dosages of Cytarabine does not contribute to its antileukaemic effectiveness in man [4].
Cas No.
69-74-9
分子式
C9H14ClN3O5
分子量
279.68
别名
Cytosine Arabinoside hydrochloride;Ara-C hydrochloride
储存和溶解度
DMSO:45mg/mL (160.9mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years