Triapine
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.
Triapine是一种有效的核糖核苷酸还原酶(ribonucleotide reductase)抑制剂,在各种肿瘤细胞系中均具有抑制效应,IC50值为1.6μM [1]。
据报道,Triapine抑制核糖核苷酸还原酶活性。Triapine通过抑制DNA合成和修复,展示了抗肿瘤活性。在小鼠M109肺癌和人A2780卵巢癌异种移植裸鼠中,Triapine抑制肿瘤生长。在L1210白血病细胞中,Triapine在很宽的剂量范围内均可以起作用[1,2]。
参考文献:
[1]. Jennifer J. Knox, Sebastien J. Hotte, Christian Kollmannsberger, Eric Winquist, Bryn Fisher, Elizabeth A. Eisenhauer .Phase II study of Triapine? in patients with metastatic renal cell carcinoma: a trial of the National Cancer Institute of Canada Clinical Trials Group (NCIC IND.161). nvestigational New Drugs .October 2007, Volume 25, Issue 5, pp 471-477
[2]Finch RA1, Liu M, Grill SP, Rose WC, Loomis R, Vasquez KM, Cheng Y, Sartorelli AC. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 195.24 |
Cas No. | 236392-56-6; 200933-27-3; 143621-35-6 |
Formula | C7H9N5S |
Synonyms | 3-AP, PAN-811, OCX191 |
Solubility | ≥83.33 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | [(E)-(3-aminopyridin-2-yl)methylideneamino]thiourea |
SDF | Download SDF |
Canonical SMILES | C1=CC(=C(N=C1)C=NNC(=S)N)N |
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 |
野生型(KB)和HU抗性(KB/HU)人类KB鼻咽癌细胞。 |
制备方法 |
在DMSO中的溶解度大于83.3 mg/mL。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
37℃ |
实验结果 |
不管酶的细胞来源如何,Triapine是一种比HU更有效的酶抑制剂,Triapine在大约低于HU 1000倍的浓度下抑制作用相当。 |
动物实验: [1] | |
动物模型 |
鼠M109肺癌和人A2780卵巢癌的小鼠异种移植物。 |
给药剂量 |
腹腔注射或静脉滴注,0.01 mL/g |
制备方法 |
溶于0.9% NaCl |
实验结果 |
Triapine显著抑制小鼠中M109肺癌的生长,与未处理的对照动物相比,每天两次给药使肿瘤生长延迟10天。人A2780卵巢癌异种移植裸鼠中,8和10 mg/kg下每天两次,Triapine显著抑制肿瘤生长。 |
注意事项 |
请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。 |
References: 1. Finch RA, Liu M, Grill SP et al. Triapine (3-aminopyridine-2-carboxaldehyde- thiosemicarbazone): A potent inhibitor of ribonucleotide reductase activity with broad spectrum antitumor activity. Biochem Pharmacol. 2000 Apr 15;59(8):983-91. |
描述 | Triapine是一种有效的核糖核苷酸还原酶抑制剂。 | |||||
靶点 | ribonucleotide reductase | |||||
IC50 |
质量控制和MSDS
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