| Size | Price | Stock | Qty |
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Plumbagin(2-Methyljuglone) is a naturally occurring naphthoquinone isolated from Plumbago zeylanica L with antimalarial and antiproliferative activities; acting as an inhibitor of human cytochrome P450 enzymes.
| ln Vitro |
In a dose-dependent manner, plumbabin (0, 5, 10, and 15 μM) activates adapters of AIDS lines, including DU145, CWR22rv1, and LNCaP[1]. (5, 20 μM) greatly reduces PC3, DU145, and CWR22rv1 cell apoptosis studies [1].
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| ln Vivo |
Plumbagin (2 mg/kg, ip, 5 days per week for 11 weeks) is a tumor suppressor of growth in athymic nude mice [1]. Plumbagin (2 mg/kg, ip, 5 days per week for 11 weeks) inhibits the expression of PKCε, inhibits JAK-2 and Stat3 phosphorylation, and activates Stat3, PCNA, VEGF and MMP-9 in mice [ 1].
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| Cell Assay |
Apoptosis Analysis[1]
Cell Types: DU145, CWR22rv1, LNCaP and RWPE-1 Cell Tested Concentrations: 0, 5, 10, and 15 μM Incubation Duration: 24 hrs (hours) Experimental Results: dose-dependent induction of apoptosis of DU145 and CWR22rv1. and LNCaP, but had no effect on RWPE-1 cells at concentrations up to 20 μM. |
| Animal Protocol |
Animal/Disease Models: Male athymic nude mice DU145 cells [1]
Doses: 2 mg/kg Route of Administration: intraperitoneal (ip) injection 3 days after cell implantation, 5 days a week. Experimental Results: Delayed tumor growth by 3 weeks and diminished tumor weight and volume in mice. |
| References | |
| Additional Infomation |
Plumbagin is a hydroxy-1,4-naphthoquinone that is 1,4-naphthoquinone in which the hydrogens at positions 2 and 5 are substituted by methyl and hydroxy groups, respectively. It has a role as a metabolite, an immunological adjuvant, an anticoagulant and an antineoplastic agent. It is a member of phenols and a hydroxy-1,4-naphthoquinone.
Plumbagin is a compound investigated for its anticancer activity. It has been found that it inactivates the Akt/NF-kB, MMP-9 and VEGF pathways. Plumbagin has been reported in Ancistrocladus cochinchinensis, Ceratostigma willmottianum, and other organisms with data available. Synthetic Plumbagin PCUR-101 is a synthetic form of the plant-derived medicinal agent, plumbagin, with potential antineoplastic activity. Plumbagin may act by inhibiting the expression of protein kinase C epsilon (PKCe), signal transducers and activators of transcription 3 phosphorylation (Stat3), protein kinase B (AKT), and certain epithelial-to-mesenchymal transition (EMT) markers, including vimentin and slug. This results in possible inhibition of proliferation in susceptible tumor cells. PKCe, Stat3, AKT, and the EMT markers vimentin and slug have been linked to the induction and progression of prostate cancer. |
| Molecular Formula |
C11H8O3
|
|---|---|
| Molecular Weight |
188.1794
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| Exact Mass |
188.047
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| CAS # |
481-42-5
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| PubChem CID |
10205
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| Appearance |
Light yellow to orange solid powder
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| Density |
1.354g/cm3
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| Boiling Point |
383.9ºC at 760 mmHg
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| Melting Point |
76-78ºC(lit.)
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| Flash Point |
200.2ºC
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| Vapour Pressure |
1.92E-06mmHg at 25°C
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| Index of Refraction |
1.63
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| LogP |
1.717
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
14
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| Complexity |
317
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
VCMMXZQDRFWYSE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C11H8O3/c1-6-5-9(13)10-7(11(6)14)3-2-4-8(10)12/h2-5,12H,1H3
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| Chemical Name |
5-hydroxy-2-methylnaphthalene-1,4-dione
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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 : ≥ 150 mg/mL (~797.11 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (11.05 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 (11.05 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 5.3141 mL | 26.5703 mL | 53.1406 mL | |
| 5 mM | 1.0628 mL | 5.3141 mL | 10.6281 mL | |
| 10 mM | 0.5314 mL | 2.6570 mL | 5.3141 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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