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阿糖胞苷 /Cytarabine {[allProObj[0].p_purity_real_show]}

货号:A568740 同义名: 阿糖胞苷 / Cytosine β-D-arabinofuranoside;Cytosine Arabinoside

Cytarabine是一种核苷类似物,诱导S期细胞周期停滞并抑制DNA聚合酶。它以16 nM的IC50抑制DNA合成,并对HSV具有抗病毒作用。阿糖胞苷还表现出抗正痘病毒的活性。

Cytarabine 化学结构 CAS号:147-94-4
Cytarabine 化学结构
CAS号:147-94-4
Cytarabine 3D分子结构
CAS号:147-94-4
Cytarabine 化学结构 CAS号:147-94-4
Cytarabine 3D分子结构 CAS号:147-94-4
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Cytarabine 纯度/质量文件 产品仅供科研

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产品名称 DNA synthesis helicase RdRp ribonucleotide reductase tRNA synthetase YB-1 其他靶点 纯度
Fexinidazole 98%
Daptomycin 98%
Blasticidin S·HCl 98%
Metronidazole 98%
Daunorubicin HCl +++

DNA synthesis, Ki: 20 nM

98%
Triglycidyl isocyanurate p53 98+%
Nedaplatin 99%+
Bendamustine 98+%
Trifluridine 98%
Robinetin 99%+
Carboplatin 99%
Cidofovir 99%
Cisplatin 99%
Cytarabine ++++

DNA synthesis, IC50: 16 nM

98%
Acelarin ++++

DNA synthesis, EC50: 0.2 nM

99%+
Oxaliplatin 98%
YK-4-279 99%+
ML216 +

BLMfull-length, IC50: 2.98 μM

BLM636-1298, IC50: 0.97 μM

99%+
RK-33 98%
Brr2-IN-3 99%+
Phen-DC3 Trifluoromethanesulfonate 98%
Favipiravir 97%
Suramin sodium salt ++

RdRp, IC50: 0.26 μM

99%+
Clofarabine ++

Ribonucleotide reductase, IC50: 65 nM

97%
Didox 98%
(E)-3-AP 97%
Halofuginone +++

prolyl-tRNA synthetase, Ki: 18.3nM

99%+
BC-LI-0186 +++

Leucyl-tRNA synthetase, Kd: 42.1 nM

Leucyl-tRNA synthetase, IC50: 46.11 nM

98%
SU056 +

YB-1, IC50: 1.73 μM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Cytarabine 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.

Cytarabine 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
HeLa human cell lines Function assay 144 h The compound was tested in vitro for antitumor activity(50% inhibition of tumor cell growth) against HeLa human cell lines after 144 hr, ID50=0.1 μM 3625714

Cytarabine 动物研究

Dose Mice: 50 mg/kg, 100 mg/kg[5] (i.p.); 20 mg/kg, 60 mg/kg[6] (s.c.)
Administration i.p., s.c.
Pharmacokinetics
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

Cytarabine 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.

Cytarabine 实验方案

计算器
存储液制备 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

Cytarabine 技术信息

CAS号147-94-4
分子式C9H13N3O5
分子量 243.21
别名 阿糖胞苷 ;Cytosine β-D-arabinofuranoside;Cytosine Arabinoside;U-19920A;NSC 287459;NSC 63878;1-β-D-Arabinofuranosylcytosine;Ara-C
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

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

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
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