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Cytarabine hydrochloride

Cytarabine hydrochloride

产品编号 T1272L   CAS 69-74-9
别名: Cytosine Arabinoside hydrochloride, Ara-C hydrochloride

Cytarabine hydrochloride 是一种核苷类似物,可导致 S 期细胞周期停滞并抑制DNA 聚合酶。Cytarabine 抑制DNA 合成,IC50为 16 nM。Cytarabine hydrochloride 对HSV 具有抗病毒作用。

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Cytarabine hydrochloride, CAS 69-74-9
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其他形式的 Cytarabine hydrochloride:
产品目录号及名称: Cytarabine hydrochloride (T1272L)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Cytarabine hydrochloride is a nucleoside analog that causes S phase cell cycle arrest and inhibits DNA polymerase. Cytarabine inhibits DNA synthesis with an IC 50 of 16 nM. Cytarabine hydrochloride has antiviral effects against HSV.
体外活性 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 with IC 50 of 16 nM compared to other acute myelogenous leukemia (AML) cells [1]. 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 [2].
体内活性 Cytarabine (250 mg/kg) also leads to 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 [3]. Cytarabine is highly effective against acute leukaemias, which causes the chCytarabineteristic 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 [4].
别名 Cytosine Arabinoside hydrochloride, Ara-C hydrochloride
分子量 279.68
分子式 C9H14ClN3O5
CAS No. 69-74-9

存储

 | Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 45mg/mL (160.9mM), Need ultrasonic

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Tobias, S.C. and R.F. Borch, Synthesis and biological evaluation of a cytarabine phosphoramidate prodrug. Mol Pharm, 2004. 1(2): p. 112-6. 2. Shepshelovich D, et al. Pharmacodynamics of cytarabine induced leucopenia: a retrospective cohort study. Br J Clin Pharmacol. 2015 Apr;79(4):685-91. 3. Besirli, C.G., et al. Cytosine arabinoside rapidly activates Bax-dependent apoptosis and a delayed Bax-independent death pathway in sympathetic neurons. Cell Death Differ, 2003. 10(9): p. 1045-58. 4. Yamauchi, H., et al., Involvement of p53 in 1-beta-D-arabinofuranosylcytosine-induced trophoblastic cell apoptosis and impaired proliferation in rat placenta. Biol Reprod, 2004. 70(6): p. 1762-7. 5. Richel, D.J., et al., Comparison of the antileukaemic activity of 5 aza-2-deoxycytidine and arabinofuranosyl-cytosine in rats with myelocytic leukaemia. Br J Cancer, 1988. 58(6): p. 730-3. 6. Renis HE. Antiviral activity of cytarabine in herpesvirus-infected rats. Antimicrob Agents Chemother. 1973 Oct;4(4):439-44.
Talviraline Cytembena AOH1996 GS-9191 Holomycin SMN-C3 Setrobuvir Apricitabine

相关化合物库

该产品包含在如下化合物库中:
FDA 上市药物库 抗癌上市药物库 核苷类化合物库 药物功能重定位化合物库 DNA 损伤和修复分子库 FDA上市及药典收录分子库 抑制剂库 抗癌活性化合物库 抗病毒库 临床期小分子药物库

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请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
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第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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Keywords

Cytarabine hydrochloride 69-74-9 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis Cytosine Arabinoside hydrochloride Ara-C hydrochloride Inhibitor inhibitor inhibit

 

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