Ellipticine
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.
Ellipticine对淋巴细胞白血病L1210细胞的IC50值为0.99 μM[1]。
植物生物碱Ellipticine抑制DNA拓扑异构酶II活性,具有抗肿瘤活性、致突变活性以及细胞毒活性。DNA拓扑异构酶II使DNA解旋,从而使另外一条未解旋的DNA穿过其中,再退火,最终引起DNA过度卷绕或卷绕不足。
体外:在哺乳动物DNA拓扑异构酶II的反应混合物中,Ellipticine促进DNA断裂。药物诱导的DNA断裂与拓扑异构酶II、DNA以及Ellipticine 3者之间形成的三元复合体相关。Ellipticine不能抑制酶介导的DNA再连接,但可以提升正向切割速率,促进DNA断裂[2]。在淋巴细胞白血病L1210细胞中,Ellipticine具有生长抑制活性,其IC50值为0.99 μM[1]。
体内:在感染伯氏疟原虫的小鼠中,采用Ellipticine进行了为期4天的抑制试验。口服给予50 mg/kg/day Ellipticine后,于第5天和第7天,Ellipticine与对照组相比具有100%抑制作用。此外,小鼠平均存活时间(MST)超过40天[3]。
临床试验:经过临床试验,几种Ellipticine衍生物的作用已被验证。然而,由于其副作用,ellipticine的临床试验暂无进展。
参考文献:
[1] Paoletti C, Cros S, Xuong ND, Lecointe P, Moisand A. Comparative cytotoxic and antitumoral effects of ellipticine derivatives on mouse L 1210 leukemia. Chem Biol Interact. 1979 Apr;25(1):45-58.
[2] Tewey KM, Chen GL, Nelson EM, Liu LF. Intercalative antitumor drugs interfere with the breakage-reunion reaction of mammalian DNA topoisomerase II. J Biol Chem. 1984 Jul 25;259(14):9182-7.
[3] Rocha e Silva LF, Montoia A, Amorim RC, Melo MR, Henrique MC, Nunomura SM, Costa MR, Andrade Neto VF, Costa DS, Dantas G, Lavrado J, Moreira R, Paulo A, Pinto AC, Tadei WP, Zacardi RS, Eberlin MN, Pohlit AM. Comparative in vitro and in vivo antimalarial activity of the indole alkaloids ellipticine, olivacine, cryptolepine and a synthetic cryptolepine analog. Phytomedicine. 2012 Dec 15;20(1):71-6.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 246.31 |
Cas No. | 519-23-3 |
Formula | C17H14N2 |
Solubility | ≥24.6 mg/mL in DMSO with gentle warming; insoluble in EtOH; insoluble in H2O |
Chemical Name | 5,11-dimethyl-6H-pyrido[4,3-b]carbazole |
SDF | Download SDF |
Canonical SMILES | CC1=C2C(NC3=CC=CC=C23)=C(C)C4=CC=NC=C14 |
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。 |
质量控制和MSDS
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