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DMAPT
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
DMAPT图片
CAS NO:870677-05-7
包装与价格：
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
DMAPT(DimethylaminoParthenolide)是Parthenolide(PTL)的水溶性类似物，是具有口服活性的NF-κB抑制剂，对原发性急性髓性白血病细胞的LD50值为1.7μM。具有潜在的抗肿瘤和抗转移作用。
Cas No.870677-05-7
别名Dimethylamino Parthenolide
Canonical SMILESC/C1=C/CC[C@]2(C)[C@H](O2)[C@]3([H])[C@](CC1)([H])[C@@H](CN(C)C)C(O3)=O
分子式C17H27NO3
分子量293.4
溶解度DMSO: 125 mg/mL (426.04 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

DMAPT (Dimethylamino Parthenolide), a water soluble analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect[1]. NF-κB[1].

DMAPT treatment decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells[2].Treatment of PC-3 and DU145 cells with 5 and 4 μM DMAPT, respectively, increases the population doubling times of PC-3 prostate cancer cells from 23.0 ± 5.0 h to 42.0 ± 3.0 h and of the DU145 cells from 20.4 ± 2.2 h to 72.5 ± 24.8 h[2]. Cell Proliferation Assay[2] Cell Line: PC-3 and DU145 cells.

Treatment with DMAPT (100 mg/kg, Oral gavage daily for 7 days) increases sensitivity of PC-3 tumor xenografts to X-rays[2].DMAPT (100 mg/kg, Oral gavage thrice weekly from 42 to 300 days since birth) treatment slows normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%[3].DMAPT further reduces the metastatic area below that of the water vehicle treatment group in lung tissues (0.10% ± 0.15 SD, 92% reduction, p = 0.0028) in TRAMP mice[3]. Animal Model: PC-3 tumor xenograft in athymic nude mice[2].

[1]. Neelakantan S, et al. Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1). Bioorg Med Chem Lett. 2009 Aug 1;19(15):4346-9. [2]. Mendonca MS, et al. DMAPT inhibits NF-κB activity and increases sensitivity of prostate cancer cells to X-rays in vitro and in tumor xenografts in vivo. Free Radic Biol Med. 2017 Nov;112:318-326. [3]. Morel KL, et al. Chronic low dose ethanol induces an aggressive metastatic phenotype in TRAMP mice, which is counteracted by parthenolide. Clin Exp Metastasis. 2018 Oct;35(7):649-661.