首页工具

购物车

3-AP

产品编号 T1982 CAS 143621-35-6

别名: NSC663249, Triapine, PAN-811, OCX191

3-AP (Triapine) 是一种新型的核糖核苷酸还原酶 M2 亚基抑制剂，也是一种放射致敏剂。

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

3-AP, CAS 143621-35-6

规格	价格/CNY	货期
2 mg	￥ 251	现货
5 mg	￥ 428	现货
10 mg	￥ 678	现货
25 mg	￥ 1,470	现货
50 mg	￥ 2,390	现货
100 mg	￥ 3,680	现货
500 mg	￥ 7,920	现货
1 mL * 10 mM (in DMSO)	￥ 453	现货

大包装超大折扣，点击咨询

选择批次

纯度: 99.75%

纯度: 99.05%

纯度: 98.95%

纯度: 97.33%

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	3-AP (Triapine) is a novel inhibitor of the M2 subunit of ribonucleotide reductase (RR).
体外活性	Triapine is a potent derivative of α-heterocyclic carboxaldehyde thiosemicarbazone (HCT) that inhibits hRRM2 and p53R2 isoforms of the M2 subunit[1]. Triapine is thought to inhibit ribonucleotide reductase through its preformed iron chelate, rather than directly by removing iron from the active site. In cells containing less topoisomerase IIα fewer DNA strand breaks will be produced, and thus topoisomerase II poisons will be less inhibitory in the K/VP.5 cell line. The IC50s for Dp44mT growth inhibition are 48±9 nM and 60±12 nM, for K562 and K/VP.5 cells, respectively. The IC50s for Triapine growth inhibition are 476±39 nM and 661±69 nM for K562 and K/VP.5 cells, respectively[2]. PKIH and DpT Fe chelators show high antiproliferative activity against a range of tumor cell lines. Dp44mT shows the greatest antitumor efficacy with an IC50 that ranged from 0.005 to 0.4 μM. The average IC50 of Dp44mT over 28 cell types is 0.03±0.01 μM, which is significantly lower than that of Triapine (average IC50: 1.41±0.37 μM)[3].
体内活性	Triapine causes a significant increase (1.7-fold) in splenic weight when expressed as a percentage of total body weight (1.02±0.06%; n=25) compared with control mice (0.6±0.03%; n=27). In the long-term group, a significant increase in heart weight is observed after Dp44mT (0.4 mg/kg per day) (0.8±0.06%; n=4) compared with control mice (0.5±0.01%; n=6). A significant decrease in the expression of Ndrg1, TfR1, and VEGF1 in the liver is noted for Dp44mT- and Triapine (12 mg/kg per day)-treated animals. The decreased expression could be related to the increased liver Fe in both Dp44mT- and Triapine-treated mice[3].
激酶实验	Ribonucleotide reductase assay: CDP reductase is assayed using Dowex 1-borate ion-exchange chromatography. The assay mixture contains 0.02 μCi of [14C]CDP (52.9 mCi/mmol), 3 mM dithiothreitol, 6 mM MgCl2, 30 mM HEPES, 5 mM ATP, 0.15 mM unlabeled CDP, and 10 μL of cellular extract in a final volume of 0.02 mL. The incubation time for the reaction is 60 min, during which time the reaction is linear.
细胞实验	Triapine is dissolved in DMSO and diluted with appropriate media[2]. An MTT assay is used to determine cell growth inhibition of CHO cells. Human leukemia K562 cells and K/VP.5 cells (a 26-fold etoposide-resistant K562-derived sub-line with decreased levels of topoisomerase IIα mRNA and protein) are maintained as suspension cultures in "MEM (Minimal Essential Medium Alpha, Invitrogen) containing 10% fetal calf serum (FCS). For growth inhibition assays, K562 and K/VP.5 cells are plated at a concentration of 1.5×105 cell/mL, and incubated 5 d with various concentrations of Dp44mT, Triapine or vehicle (DMSO) for 48 h, after which cells are counted on a model ZBF Coulter counter. The IC50 growth inhibitory concentration for each cell line is calculated from a non-linear least-squares fit to a 2-parameter logistic equation[2].

别名	NSC663249, Triapine, PAN-811, OCX191
分子量	195.24
分子式	C7H9N5S
CAS No.	143621-35-6

存储

store at low temperature　|　Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 50 mg/mL (256.1 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	5.1219 mL	25.6095 mL	51.219 mL	128.0475 mL
	5 mM	1.0244 mL	5.1219 mL	10.2438 mL	25.6095 mL
	10 mM	0.5122 mL	2.561 mL	5.1219 mL	12.8048 mL
	20 mM	0.2561 mL	1.2805 mL	2.561 mL	6.4024 mL
	50 mM	0.1024 mL	0.5122 mL	1.0244 mL	2.561 mL
	100 mM	0.0512 mL	0.2561 mL	0.5122 mL	1.2805 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Martin LK, et al. A dose escalation and pharmacodynamic study of Triapine and radiation in patients with locally advanced pancreas cancer. Int J Radiat Oncol Biol Phys. 2012 Nov 15;84(4):e475-81.

文献引用

1. Wang R, Xie S, Zhu S, et al. Targeting matrix metallopeptidase 2 by hydroxyurea selectively kills acute myeloid mixed-lineage leukemia. Cell Death Discovery. 2022, 8(1): 1-10

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

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。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

3-AP 143621-35-6 Cell Cycle/Checkpoint DNA Damage/DNA Repair DNA/RNA Synthesis NSC663249 inhibit PAN 811 Inhibitor PAN811 Triapine 3 AP PAN-811 OCX 191 3AP OCX191 NSC-663249 NSC 663249 NSC# 663249 OCX-191 inhibitor

我们的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

沪公网安备 31010602006700号

陶术

生物

TargetMol^®中国区唯一合作伙伴

点击进入陶术生物官网

联系我们

电话：

400-820-0310

邮箱：

service@tsbiochem.com

QQ：

2881945090（终端用户）

2885109491（经销商）

经销：

终端：

地址：

上海市静安区江场三路238号8楼

3-AP

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords