生物活性

• 描述Cytarabine (Ara-C) is an antineoplastic and antileukemic agent in current clinical treatment. Cytarabine belongs to a class of nucleoside-analogue antimetabolite, which can enter into cells and be phosphorylated by deoxynucleoside salvage pathway and produce their activity by being incorporated into DNA during replication or repair, leading to inhibition of chain extension^[1]. Cytarabine, combined with other drugs, is mainly used in the treatment for acute lymphoblastic leukemia (ALL), acute myeloid leukemia (AML) and chronic myelogenous leukemia (CML) (see https://www.fda.gov/), also can be used in treatment for other cancer. Cytarabine can inhibit DNA synthesis mainly through being incorporated into cellular DNA by both repair and replication synthesis^[2]. Cytarabine can induce apoptosis, s phase arrest, as well as cell growth inhibition^[3]. Cytarabine is usually used in long-term neuron culture to reduce glial cells and enhance neurons for its mitotic inhibition^[4].
• 作用机制Cytarabine, as nucleoside analogue, can inhibit DNA synthesis mainly through being incorporated into cellular DNA by both repair and replication synthesis.

• 动物研究
  剂量	Mice: 50 mg/kg, 100 mg/kg[5] (i.p.); 20 mg/kg, 60 mg/kg[6] (s.c.)
  给药途径	i.p., s.c.
  动物药代数据	Animal Nude mice[7] Dogs[8] Dose 2466 μmol/kg 25 mg/m2/h Administration s.c. T1/2 0.29 h Cmax 1.70 ± 0.66 μg/ml AUC0→∞ 1553 nmol·h/mL AUC 11.39 ± 3.37 h·μg/ml