DMAPT (Synonyms: Dimethylamino Parthenolide)
目录号: PL07790 纯度: ≥98.0%
CAS No. :870677-05-7
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中文名称
DMAPT
中文别名
DMAPT
英文名称
DMAPT
英文别名
DMAPT
Cas No.
870677-05-7
分子式
C17H27NO3
分子量
293.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
DMAPT (Dimethylamino Parthenolide) 是Parthenolide (PTL) 的类似物,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1.7 μM。具有潜在的抗肿瘤和抗转移作用。
生物活性
DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD 50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect.
性状
Solid
IC50 & Target[1][2]
NF-κB.
体外研究(In Vitro)
DMAPT treatment decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.-t
体内研究(In Vivo)
Treatment with DMAPT (100 mg/kg, Oral gavage daily for 7 days) increases sensitivity of PC-3 tumor xenografts to X-rays.
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%.
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.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[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.
溶解度数据
In Vitro: DMSO : 125 mg/mL (426.04 mM; Need ultrasonic)H2O : 1.1 mg/mL (3.75 mM; ultrasonic and warming and heat to 40°C)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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