DMAPT-Dimethylamino-Parthenolide-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDMAPTCat. No.: HY-16172CAS No.: 870677-05-7Synonyms: Dimethylamino Parthenolide分式: CHNO分量: 293.4作靶點(diǎn): NF-B作通路: NF-B儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (426.04 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 3.4083 mL 17.0416 mL 34.0832 mL5 mM 0.6817 mL 3.4083 mL 6.8166 mL10 mM 0.3408 mL 1.7042 mL 3.4083 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件

3、，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.08 mg/mL (7.09 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (7.09 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/3 Master of Small Molecules 您

4、邊的抑制劑師www.MedChemESolubility: 2.08 mg/mL (7.09 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 DMAPT (Dimethylamino Parthenolide)Parthenolide (PTL) 的溶性類似物， 具有服活性的 NF-B 抑制劑，對(duì)原發(fā)性急性髓性病細(xì)胞的LD50 值為1.7 M。具有潛在的抗腫瘤和抗轉(zhuǎn)移作。IC50 & Target NF-B 1.體外研究 DMAPT treatment decreased constitutive NF-B binding activity, inhibit

5、s cell proliferation and viability of PC-3and DU145 cells 2.Treatment of PC-3 and DU145 cells with 5 and 4 M DMAPT, respectively, increases thepopulation doubling times of PC-3 prostate cancer cells from 23.0 5.0 h to 42.0 3.0 h and of the DU145cells from 20.4 2.2 h to 72.5 24.8 h 2.Cell Proliferati

6、on Assay 2Cell Line: PC-3 and DU145 cells.Concentration: PC-3 cells (0, 2.5, 5 M), DU145 cells (0 and 4 M).Incubation Time: 24 and 48 hours.Result: Decreased constitutive NF-B binding activity, inhibits cell proliferation and viability ofPC-3 and DU145 cells.體內(nèi)研究Treatment with DMAPT (100 mg/kg, Oral

7、 gavage daily for 7 days) increases sensitivity of PC-3 tumorxenografts to X-rays 2.DMAPT (100 mg/kg, Oral gavage thrice weekly from 42 to 300 days since birth) treatment slows normaltumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20% 3.DMAPT further reduces the met

8、astatic 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.Dosage: 100 mg/kg.Administration: Oral gavage daily for 7 days.Result: Increased sensitivity of PC-3 tumor

9、xenografts to X-rays.Animal Model: Six-week-old male TRAMP mice 3.Dosage: 100 mg/kg.Administration: Oral gavage thrice weekly from 42 to 300 days since birth.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEResult: Slowed normal tumor development in TRAMP mice, extending the time-to-palpableprostate

10、 tumor by 20%.REFERENCES1. Neelakantan S, et al. Aminoparthenolides as novel anti-leukemic agents: Discovery of the NF-kappaB inhibitor, DMAPT (LC-1). BioorgMed Chem Lett. 2009 Aug 1;19(15):4346-9.2. Mendonca MS, et al. DMAPT inhibits NF-B activity and increases sensitivity of prostate cancer cells

11、to X-rays in vitro and in tumorxenografts 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 byparthenolide. Clin Exp Metastasis. 2018 Oct;35(7):649-661.McePdfHeightCaution: Product has not b