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Cytarabine

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Chemical Structure| 147-94-4 同义名 : 阿糖胞苷 ;Cytosine β-D-arabinofuranoside;Cytosine Arabinoside;U-19920A;NSC 287459;NSC 63878;1-β-D-Arabinofuranosylcytosine;Ara-C
CAS号 : 147-94-4
货号 : A568740
分子式 : C9H13N3O5
纯度 : 98%
分子量 : 243.21
MDL号 : MFCD00066487
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 16 mg/mL(65.78 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 45 mg/mL(185.02 mM)，配合低频超声助溶
动物实验配方：
生物活性
靶点

  • DNA synthesis

    DNA synthesis, IC50:16 nM
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.
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
CCRF-CEM cell line Function assay Inhibit the replication of CCRF-CEM cell line in vitro, ED50=5 nM. 1995894
CCRF-CEM cell lines Function assay 72 h Concentration required to inhibit replication of CCRF-CEM cell lines by 50% after 72 hr incubation, ED50=6 nM. 1652024
CCRF-CEM human leukemic lymphoblastoid cell lines Cytotoxic assay Cytotoxicity against CCRF-CEM human leukemic lymphoblastoid cell lines, IC50=20 nM. 6827546
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.11mL

0.82mL

0.41mL

20.56mL

4.11mL

2.06mL

41.12mL

8.22mL

4.11mL
参考文献

[1]Johnson SA, et al. Nucleoside analogues in the treatment of haematological malignancies. Expert Opin Pharmacother. 2001 Jun;2(6):929-43.

[2]Wills P, Hickey R, et al. A novel in vitro model system for studying the action of ara-C. Cancer Chemother Pharmacol. 1996;38(4):366-72.

[3]Wang X, Chen Z, et al. Chemotherapy-induced differential cell cycle arrest in B-cell lymphomas affects their sensitivity to Wee1 inhibition. Haematologica. 2018 Mar;103(3):466-476.

[4]Schwieger J, Esser KH, et al. Establishment of a long-term spiral ganglion neuron culture with reduced glial cell number: Effects of AraC on cell composition and neurons. J Neurosci Methods. 2016 Aug 1;268:106-16.

[5]Zuber J, Radtke I, et al. Mouse models of human AML accurately predict chemotherapy response. Genes Dev. 2009 Apr 1;23(7):877-89.

[6]Scatena CD, Kumer JL, et al. Voreloxin, a first-in-class anticancer quinolone derivative, acts synergistically with cytarabine in vitro and induces bone marrow aplasia in vivo. Cancer Chemother Pharmacol. 2010 Oct;66(5):881-8.

[7]Bayne WF, Mayer LD, et al. Pharmacokinetics of CPX-351 (cytarabine/daunorubicin HCl) liposome injection in the mouse. J Pharm Sci. 2009 Jul;98(7):2540-8.

[8]Early PJ, Crook KI, et al. Plasma and serum concentrations of cytarabine administered via continuous intravenous infusion to dogs with meningoencephalomyelitis of unknown etiology. J Vet Pharmacol Ther. 2017 Aug;40(4):411-414.