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Cytarabine.

(Synonyms: 阿糖胞苷; Cytosine β-D-arabinofuranoside; Cytosine Arabinoside; Ara-C)
目录号: PC10316 纯度: ≥98%
Cytarabine是一种用于治疗急性髓性白血病的化疗药物,抑制DNA 合成的IC50为16 nM。
CAS No. :147-94-4
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中文名称
Cytarabine.
中文别名
阿糖胞苷;1-beta-D-阿拉伯呋喃糖基-4-氨基-2(1H)-嘧啶酮;胞嘧啶-β-D-呋喃阿拉伯糖苷;阿拉伯糖胞嘧啶;胞嘧啶阿拉伯糖苷;阿拉伯呋喃糖基胞嘧啶;阿拉伯糖基胞嘧啶;1-BETA-D-阿拉伯呋喃糖基-4-氨基-2(1H)-嘧啶;海綿胞嘧啶;胞嘧啶核苷(胞苷);Cutosine β-D- 阿糖胞苷;Cytarabine 阿糖胞苷;阿糖胞苷 EP标准品;阿糖胞苷 USP标准品;阿糖胞苷-13C-15N2;阿糖胞苷-13C3;阿糖胞苷标准品;阿糖胞嘧啶;阿糖胞嘧啶(阿糖胞苷);阿扎胞苷;胞嘧啶 β-D-阿拉伯呋喃糖苷;羟基喜树碱;(β-D-阿拉伯呋喃糖基)胞嘧啶;1-β-D-阿拉伯呋喃糖基-4-氨基-2(1H)-嘧啶酮;阿哌沙班;阿糖呋喃胞嘧啶;胞嘧啶-1-Β-D(+)-阿拉伯呋喃酐;胞嘧啶β-D-呋喃阿拉伯糖苷;胞嘧啶-β-D-呋喃阿拉伯糖苷,1-β-D-阿拉伯呋喃糖基-4-氨基-2(1H)-嘧啶酮;4-氨基-1-β-D-阿拉伯呋喃糖基-2(1H)-嘧啶酮;阿糖胞苷(标准品);胞嘧啶 β-D-呋喃阿拉伯糖苷;阿糖胞苷, 97+%
英文名称
Cytarabine
英文别名
4-Amino-1-((2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)pyrimidin-2(1H)-one;1-B-D-ARABINOFURANOSYL CYTOSIN;1-[BETA-D-ARABINOFURANOSYL]CYTOSINE;2'-ARACYTIDINE;4-AMINO-1-BETA-D-ARABINOFURANOSYL-2(1H)-PYRIMIDINONE;ARABINOCYRIDINE;ARABINOFURANOSYLCYTOSINE;ARABINOSYLCYTOSINE;CYTARABINE;CYTOSINE-1-BETA-D(+)-ARABINOFURANOSIDE;CYTOSINE ARABINOSIDE;CYTOSINE BETA-D-ARABINOFURANOSIDE;1-arabinofuranosylcytosine;1-beta-arabinofuranosylcytosine;1-beta-d-arabinofuranosyl-4-amino-2(1h)pyrimidinone;1-beta-d-arabinofuranosyl-cytosin;1-beta-d-arabinosyl-cytosin;1-beta-d-arabinosylcytosine;Cytosine β-D-arabinofuranoside;1-β-D-Arabinofuranosylcytosine;Cytarabine hydrochloride;(β-D-Arabinofuranosyl)cytosine;4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one;4-Amino-1-β-D-arabinofuranosyl-2(1H)-pyrimidinone;Ara-C;Arabinocytidine;udicil;Iretin;arafcyt;cytosar;Citozar;Ara-cell;arabitin;aracytin;Cytarabin;Tarabine;Alexan;Cytosar-U;1-beta-D-Arabinofuranosylcytosine;Cytarabina;Depocyt;DepoCyte;Citarabina;Cytarabinum;Aracytine;Aracytidine;Cytosinearabinoside;Cytarabinoside;Cytosine-beta-D-arabinofuranoside;Cytonal;Cytosine arabinofuranoside;beta-D-Arabinosylcytosine;Depocyt (liposomal);Cytarabinum [INN-
Cas No.
147-94-4
分子式
C9H13N3O5
分子量
243.22
包装储存
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
详情描述

Cytarabine是一种用于治疗急性髓性白血病的化疗药物,抑制DNA 合成的IC50为16 nM。

生物活性

Cytarabine, a nucleoside analog, causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC50 of 16 nM. Cytarabine has antiviral effects against HSV. Cytarabine shows anti-orthopoxvirus activity.

性状

Solid

IC50 & Target[1][2]

Microbial Metabolite

 

HSV-1

 

体外研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
ClinicalTrial
结构分类
来源

Xerocomus nigromaculatus

参考文献
溶解度数据
体外研究: 

H2O : 48 mg/mL (197.35 mM; Need ultrasonic)

DMSO : 17.3 mg/mL (71.13 mM; Need ultrasonic and warming)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.1115 mL 20.5575 mL 41.1150 mL
5 mM 0.8223 mL 4.1115 mL 8.2230 mL
10 mM 0.4112 mL 2.0558 mL 4.1115 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: PBS

    Solubility: 100 mg/mL (411.15 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.55 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (8.55 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (8.55 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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