| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
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| Targets |
NF-κB[1].
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| ln Vitro |
In PC-3 and DU145 cells, DMAPT treatment decreased constitutive NF-κB binding activity and impaired cell proliferation and viability [2]. The PC-3 prostate cancer cells' population doubling time rose from 23.0 ± 5.0 hours to 42.0 ± 3.0 hours and the DU145 cells' population doubling time from 20.4 ± 2.2 hours to 42.0 ± 3.0 hours after being treated with 5 and 4 μM DMAPT, respectively. Reaching 72.5 ± 24.8 hours [2].
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| ln Vivo |
PC-3 tumor xenografts are more susceptible to X-rays when treated with DMAPT (100 mg/kg, daily oral gavage for 7 days) [2]. In TRAMP mice, treatment with DMAPT (100 mg/kg, given by oral gavage three times a week from days 42 to 300 of life) slowed the normal tumor development and increased the time to palpable prostate tumors by 20% [3]. DMAPT additionally showed that the lung tissue metastatic area was smaller in TRAMP mice [3] compared to the group treated with water vehicles (0.10% ± 0.15 SD, 92% decrease, p=0.0028).
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| Cell Assay |
Cell Types: PC-3 and DU145 cells.
Tested Concentrations: PC-3 cells (0, 2.5, 5 μM), DU145 cells (0 and 4 μM). Incubation Duration: 24 and 48 hrs (hours). Experimental Results: diminished constitutive NF -κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells. |
| Animal Protocol |
Animal/Disease Models: PC-3 tumor xenograft in athymic nude mice[2].
Doses: 100 mg/kg. Route of Administration: po (oral gavage) daily for 7 days. Experimental Results: Increased sensitivity of PC-3 tumor xenografts to X-rays. Animal/Disease Models: Sixweeks old male TRAMP mice[3]. Doses: 100 mg/kg. Route of Administration: po (oral gavage) thrice weekly from 42 to 300 days since birth. Experimental Results: 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.
[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. [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. |
| Molecular Formula |
C17H27NO3
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|---|---|
| Molecular Weight |
293.40
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| CAS # |
791595-09-0
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| Related CAS # |
(S)-DMAPT;870677-05-7
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| Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO :~125 mg/mL (~426.04 mM)
H2O :~1.1 mg/mL (~3.75 mM; ultrasonic and warming and heat to 40°C) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (7.09 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.4083 mL | 17.0416 mL | 34.0832 mL | |
| 5 mM | 0.6817 mL | 3.4083 mL | 6.8166 mL | |
| 10 mM | 0.3408 mL | 1.7042 mL | 3.4083 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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