| Identification | Back Directory | [Name]
Oxireno[9,10]cyclodeca[1,2-b]furan-9(1aH)-one, 8-[(dimethylamino)methyl]-2,3,6,7,7a,8,10a,10b-octahydro-1a,5-dimethyl-, (1aR,4E,7aS,8R,10aS,10bR)- | [CAS]
791595-09-0 | [Synonyms]
Oxireno[9,10]cyclodeca[1,2-b]furan-9(1aH)-one, 8-[(dimethylamino)methyl]-2,3,6,7,7a,8,10a,10b-octahydro-1a,5-dimethyl-, (1aR,4E,7aS,8R,10aS,10bR)- | [Molecular Formula]
C17H27NO3 | [MOL File]
791595-09-0.mol | [Molecular Weight]
293.4 |
| Chemical Properties | Back Directory | [Boiling point ]
419.7±45.0 °C(Predicted) | [density ]
1.061±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMF: Miscible,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: Miscible,Ethanol: 30 mg/ml | [form ]
A crystalline solid | [pka]
8.74±0.28(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
DMAPT (Dimethylamino Parthenolide), an analogue of Parthenolide (PTL), is an oral active NF-κB inhibitor, with a LD50 of 1.7 μM for cell population in AML cells. Has potential anti-cancer and anti-metastatic effect[1]. | [in vivo]
Treatment with DMAPT (100 mg/kg, Oral gavage daily for 7 days) increases sensitivity of PC-3 tumor xenografts to X-rays[2].
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%[3].
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[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 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. | | Result: | Slowed normal tumor development in TRAMP mice, extending the time-to-palpable prostate tumor by 20%. |
| [References]
[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. DOI:10.1016/j.bmcl.2009.05.092
[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. DOI:10.1016/j.freeradbiomed.2017.08.001
[3] Morel KL, et al. Chronic low dose ethanol induces an aggressive metastatic phenotype in TRAMP mice, which is counteracted by parthenolide. Clin Exp Metastasis. 2018 Oct;35(7):649-661. DOI:10.1007/s10585-018-9915-9 |
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