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DMAPT (Synonyms: Dimethylamino Parthenolide)

Cat. No.: HY-16172 Purity: >98.0%
Handling Instructions

DMAPT (Dimethylamino Parthenolide), a water soluble 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.

For research use only. We do not sell to patients.

DMAPT Chemical Structure

DMAPT Chemical Structure

CAS No. : 870677-05-7

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10 mM * 1 mL in DMSO USD 165 In-stock
Estimated Time of Arrival: December 31
5 mg USD 150 In-stock
Estimated Time of Arrival: December 31
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Description

DMAPT (Dimethylamino Parthenolide), a water soluble 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].

IC50 & Target

NF-κB[1].

In Vitro

DMAPT treatment decreased constitutive NF-κB binding activity, inhibits cell proliferation and viability of PC-3 and DU145 cells[2].
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[2].

Cell Proliferation Assay[2]

Cell 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 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%.
Molecular Weight

293.40

Formula

C₁₇H₂₇NO₃

CAS No.

870677-05-7

SMILES

C/C1=C/CC[[email protected]]2(C)[[email protected]](O2)[[email protected]]3([H])[[email protected]](CC1)([H])[[email protected]@H](CN(C)C)C(O3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (426.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.09 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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DMAPT
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