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Cytarabine

CAS No. : 147-94-4

MCE 站：Cytarabine

产品活性：Cytarabine 是一种核苷类似物，可引起 S 期细胞周期停滞并抑制 DNA聚合酶。Cytarabine 抑制DNA 合成的IC₅₀为16 nM。Cytarabine 对 HSV 具有抗病毒作用。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection  |  Autophagy  |  Apoptosis  |  Metabolic Enzyme/Protease

作用靶点：DNA/RNA Synthesis  |  Nucleoside Antimetabolite/Analog  |  HSV  |  Autophagy  |  Endogenous Metabolite  |  Apoptosis

In Vitro: 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 compared to other acute myelogenous leukemia (AML) cells with IC₅₀ of 16 nM. 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.

In Vivo: Cytarabine (250 mg/kg) also causes 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. Cytarabine is highly effective against acute leukaemias, which causes the Cytarabine teristic 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.

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