DMAPT 是一种具有口服活性的NF-Κb抑制剂,是一种 Parthenolide (PTL) 的类似物,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。
产品描述
DMAPT is a water-soluble analogue of Parthenolide (PTL). It is an orally active NF-κB inhibitor with an LD50 of 1.7 μM on primary acute myeloid leukemia cells.
体外活性
DMAPT treatment reduced the constitutive NF-κB binding activity and inhibited the proliferation and viability of PC-3 and DU145 cells. Treatment of PC-3 and DU145 cells with 5 and 4 μM DMAPT, respectively, increased the population doubling time of PC-3 prostate cancer cells from 23.0±5.0 h to 42.0±3.0 h, while the population doubling time of DU145 cells increased from 20.4±2.2 h By 72.5±24.8 hours.
体内活性
DMAPT (100 mg/kg, oral gavage daily for 7 days) treatment can increase the sensitivity of PC-3 tumor xenografts to X-rays. DMAPT (100 mg/kg, 42 to 300 days from birth, oral gavage three times a week) treatment can slow the normal tumor development of TRAMP mice and prolong the reachable prostate tumor time by 20%. DMAPT further reduced the lung tissue transfer area of TRAMP mice to below the water vehicle treatment group (0.10%±0.15 SD, 92% reduction, p = 0.0028)[3].
Cas No.
870677-05-7
分子式
C17H27NO3
分子量
293.4
别名
Dimethylamino Parthenolide;DMAPT
储存和溶解度
DMSO:100 mg/mL (340.83 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years