DMAPT (C09-1125-579)

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 effectIn VitroDMAPT treatment decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells. ?/nTreatment 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell Line: PC-3 and DU145 cells. Concentration: PC-3 cells (0, 2.5, 5 μM), DU145 cells (0 and 4 μM). Incubation Time: 24 and 48 hours. Result: Decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells.In VivoTreatment with DMAPT (100 mg/kg, Oral gavage daily for 7 days) increases sensitivity of PC-3 tumor xenografts to X-rays. ?/nDMAPT (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%. ?/nDMAPT 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: PC-3 tumor xenograft in athymic nude mice. Dosage: 100 mg/kg. Administration: Oral gavage daily for 7 days. Result: Increased sensitivity of PC-3 tumor xenografts to X-rays. Animal Model: Six-week-old male TRAMP mice. Dosage: 100 mg/kg. Administration: Oral gavage thrice weekly from 42 to 300 days since birth. Result: Slowed normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%.Form:SolidIC50& Target:NF-κB. Specification: ≥98.0% Molecular Formula: C17H27NO3 Molecular Weight: 293.4