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Cytarabine (阿糖胞苷) 返回列表頁

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參考價:500

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型號
HY-13605
品牌
MCE
廠商性質(zhì)
代理商
所在地
杭州市

規(guī)格

100mg 500元 10000支可售

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產(chǎn)品簡介

CAS號	147-94-4	產(chǎn)地	國產(chǎn)
規(guī)格	100mg	級別	化工級
證書	ISO系列證書

Cytarabine 是一種核苷類似物，可引起 S 期細胞周期停滯并抑制 DNA聚合酶。Cytarabine 抑制DNA 合成的IC50為16 nM。Cytarabine 對 HSV 具有抗病毒作用。Cytarabine 具有抗正痘活性。

詳情介紹

Cytarabine (Synonyms: 阿糖胞苷; Cytosine β-D-arabinofuranoside; Cytosine Arabinoside; Ara-C)

Cytarabine 是一種核苷類似物，可引起 S 期細胞周期停滯并抑制 DNA聚合酶。Cytarabine 抑制DNA 合成的IC₅₀為16 nM。Cytarabine 對 HSV 具有抗病毒作用。Cytarabine 具有抗正痘活性。

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.

體外研究(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^[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].

體內(nèi)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^[3]. 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^[4].

分子量：243.22

性狀：Solid

Formula：C₉H₁₃N₃O₅

CAS 號：147-94-4

中文名稱：阿糖胞苷；阿糖胞嘧啶

來源：Xerocomus nigromaculatus

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性數(shù)據(jù)

In Vitro:

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

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

配制儲備液

濃度溶劑體積質(zhì)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

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： PBS
Solubility: 100 mg/mL (411.15 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
2.

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (8.55 mM); Clear solution
3.

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (8.55 mM); Clear solution
4.

請依序添加每種溶劑： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (8.55 mM); Clear solution

參考文獻

[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.  [Content Brief]
[2]. 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.  [Content Brief]
[3]. 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.  [Content Brief]
[4]. 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.  [Content Brief]
[5]. Shepshelovich D, et al. Pharmacodynamics of cytarabine induced leucopenia: a retrospective cohort study. Br J Clin Pharmacol. 2015 Apr;79(4):685-91.  [Content Brief]
[6]. Renis HE. Antiviral activity of cytarabine in herpesvirus-infected rats. Antimicrob Agents Chemother. 1973 Oct;4(4):439-44.  [Content Brief]
[7]. Gruffaz M, Zhou S, Vasan K, et al. Repurposing Cytarabine for Treating Primary Effusion Lymphoma by Targeting Kaposi's Sarcoma-Associated Herpesvirus Latent and Lytic Replications. mBio. 2018;9(3):e00756-18. Published 2018 May 8.  [Content Brief]
[8]. Smee DF, et al. A review of compounds exhibiting anti-orthopoxvirus activity in animal models. Antiviral Res. 2003 Jan;57(1-2):41-52.  [Content Brief]
注：產(chǎn)品僅用于科研