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DMAPT
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DMAPT
CAS No. : 870677-05-7
MCE 站:DMAPT
产品活性: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。
研究领域:NF-κB
作用靶点:NF-κB
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.
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.
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