Cytarabine
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Cytarabine (AraC),一种脱氧胞苷的类似物,是治疗急性髓性白血病(AML)的最有效细胞毒性药物,通过抑制DNA和RNA聚合酶的功能来阻断DNA合成[1]。
Cytarabine嵌合到DNA中,通过抑制DNA和RNA聚合酶的功能来阻断DNA合成。AraC活化的最重要步骤是经磷酸化生成单磷酸形式,这是由脱氧胞苷激酶(dCK)催化而得。
在AraC敏感的大鼠白血病细胞中,单一表达失活或剪切dCK形式使细胞耐受AraC的细胞毒性效应。据报道,Ara-C还导致胎盘生长迟缓,诱导细胞凋亡,以及抑制胎盘迷路区域中的细胞增殖。给孕鼠注射Ara-C后,从1到48小时对胎盘进行了检查。胎盘迷路区域中的滋养层细胞凋亡自注入后3小时起增加,在第6小时达到峰值,于第48小时恢复到控制水平。在胎盘迷路区域中p53蛋白的免疫反应性显著增强,在治疗后3小时达到峰值,但逆转录聚合酶链反应检测表明p53的mRNA表达没有增加[1,2]。
对40例持续5天接受每天每平方米1000 mg Cytarabine、8 mg Mitoxantrone和100 mg Etoposide的患者进行了一项回顾性分析。得到30%的缓解率和11.2个月的平均缓解持续时间。在单因素分析中,对比≥第二次复发(P = 0.02),第一次复发的患者具有更长的总生存期[3]。
参考文献:
[1]. Veuger MJT, Heemskerk MHM, Honders MW, et al. Functional role of alternatively spliced deoxycytidine kinase in sensitivity to cytarabine of acute myeloid leukemic cells. Blood, 2002, 99(4): 1373-1380.
[2]. Yamauchi H, Katayama K, Ueno M, et al. Involvement of p53 in 1-beta-D-arabinofuranosylcytosine-induced trophoblastic cell apoptosis and impaired proliferation in rat placenta. Biology of Reproduction, 2004, 70(6): 1762-1767.
[3]. Liedtke M, Dunn T, Dinner S, et al. Salvage therapy with mitoxantrone, etoposide and cytarabine in relapsed or refractory acute lymphoblastic leukemia. Leukemia Research, 2014, 38(12): 1441-1445.
- 1. Emmanuelle Supper, Saskia Rudat, et al. "Cut-like homeobox 1 (CUX1) tumor suppressor gene haploinsufficiency induces apoptosis evasion to sustain myeloid leukemia." Nat Commun. 2021 Apr 30;12(1):2482. PMID: 33931647
- 2. Zhijun Liu, Himani Nailwal, et al. "A class of viral inducer of degradation of the necroptosis adaptor RIPK3 regulates virus-induced inflammation." Immunity. 2021 Feb 9;54(2):247-258.e7. PMID: 33444549
- 3. Lin KH, Xie A, et al. "Systematic Dissection of the Metabolic-Apoptotic Interface in AML Reveals Heme Biosynthesis to Be a Regulator of Drug Sensitivity." Cell Metab. 2019 Feb 5. pii: S1550-4131(19)30011-7. PMID: 30773463
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 243.2 |
Cas No. | 147-94-4 |
Formula | C9H13N3O5 |
Solubility | insoluble in EtOH; ≥28.6 mg/mL in H2O; ≥11.73 mg/mL in DMSO |
Chemical Name | 4-amino-1-[(2R,3S,4S,5R)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]pyrimidin-2-one |
SDF | Download SDF |
Canonical SMILES | C1=CN(C(=O)N=C1N)C2C(C(C(O2)CO)O)O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验 [1]: | |
细胞系 |
大鼠交感神经元 |
溶解方法 |
该化合物在DMSO中的溶解度有限。若获取更高浓度的溶液,可在37℃下孵育10分钟,随后在超声波浴中摇匀。-20℃以下可储存数月。 |
反应条件 |
10 μM |
应用 |
Cytarabine (10 μM)明显诱导大鼠交感神经元细胞凋亡,100μM显示出最高毒性,孵育84小时引起80%以上的神经元死亡,并引起线粒体细胞色素c的释放和caspase-3的活化。 |
动物实验 [2]: | |
动物模型 |
怀孕Slc:Wistar大鼠 |
给药剂量 |
腹腔注射,250 mg/kg |
应用 |
在怀孕Slc:Wistar大鼠的胎盘迷宫区,Cytarabine (250 mg/kg)引起胎盘生长迟缓,增加胎盘滋养细胞凋亡,治疗后3小时增加,并在6小时达到峰值,在48小时恢复到对照水平,Cytarabine显著增强p53蛋白及p53转录靶基因如p21、cyclinG1和fas以及caspase-3活性。 |
注意事项 |
由于实验环境的不同,实际溶解度可能与理论值略有不同,请测试室内所有化合物的溶解度。 |
References: [1]. Besirli C G, Deckwerth T L, Crowder R J, et al. Cytosine arabinoside rapidly activates Bax-dependent apoptosis and a delayed Bax-independent death pathway in sympathetic neurons[J]. Cell death and differentiation, 2003, 10(9): 1045. [2]. Yamauchi H, Katayama K, Ueno M, et al. Involvement of p53 in 1-β-D-arabinofuranosylcytosine-induced trophoblastic cell apoptosis and impaired proliferation in rat placenta[J]. Biology of reproduction, 2004, 70(6): 1762-1767. |
质量控制和MSDS
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