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D-609 (D609) is a novel, competitive and potent phospholipase C inhibitor with the potential to be used for the treatment of pancreatic cancer. It inhibits phosphatidyl choline-specific phospholipase C (PC-PLC) with Ki of 6.4 μM.
| ln Vitro |
D609 at 100 μM for two hours greatly reduces edema in several cell lines [2]. After activating caspase-3 at 200 μM for two hours, D609 (100 μM; two hours) at 50, 100 μM significantly inhibited BrdU in BV-2 astrocytes. It occurs annually and results in a decrease in the number of cells in the S phase and an accumulation of cells in the G1 phase [2]. 100 μM; for two hours, then for two more hours or for twenty-two hours without D609) raises ceramide levels, boosts p21 expression, and causes phosphorylated Rb to drop [2].
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| ln Vivo |
In apoE-/-mice, D609 (2.5, 10 mg/kg/day; i.p.; for 6 weeks) inhibits the progression of preexisting atherosclerotic lesions, changing the event component to a more stable phenotype [3 LPS administered intratracheally (30 mg/kg; i.p.; single dose) 30 minutes prior to LPS (3 mg/kg) prevents LPS-induced pulmonary hypertension in Island Wistar [4]. C57BL/6 WT and apoE−/− 26-week-old mice [3]
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| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: RAW 264.7 macrophages, N9 and BV-2 microglia, and DITNC1 astrocytes Tested Concentrations: 100 μM Incubation Duration: 2 hrs (hours) Experimental Results: Dramatically attenuated RAW 264.7 macrophages , N9 and BV-2 microglia, and DITNC1 astrocytes without affecting cell viability. Apoptosis analysis[2] Cell Types: BV-2 Cell Tested Concentrations: 50, 100 and 200 μM Incubation Duration: 2 hrs (hours) Experimental Results: Activation of caspase-3 in a dose- and time-dependent manner. Cell cycle analysis [2] Cell Types: BV-2 Cell Tested Concentrations: 100 μM Incubation Duration: 2 hrs (hours) Experimental Results: Dramatically inhibited the incorporation of BrdU in BV-2 microglia, resulting in G1 phase cell aggregation and S phase cell number reduction phase. Western Blot Analysis[2] Cell Types: BV-2 Cell Tested Concentrations: 100 μM Incubation Duration: 2 hrs (hours) Experimental Results: Increased ceramide levels, upregulation of p21 expression and resulting reduction in phospho-Rb. |
| Animal Protocol |
Animal/Disease Models: 26weeks old apoE−/− and C57BL/6 WT mice[3]
Doses: 2.5, 10 mg/kg Route of Administration: IP; per day for 6 weeks Experimental Results:Inhibited the progression of preexisting atherosclerotic lesions in apoE−/− mice and changed the lesion composition into a more stable phenotype. Dramatically diminished the aortic endothelial expression of the vascular cell adhesion molecule-1 and the intercellular adhesion molecule-1. |
| References |
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| Molecular Formula |
C11H15KOS2
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|---|---|
| Molecular Weight |
266.4583
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| Exact Mass |
266.02
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| CAS # |
83373-60-8
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| Related CAS # |
83373-60-8 (K+); 145764-52-9 (free);
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| PubChem CID |
4234241
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| Appearance |
White to off-white solid powder
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| Density |
1.24 g/cm3
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| Boiling Point |
303.8ºC at 760 mmHg
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| Flash Point |
137.5ºC
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| LogP |
3.31
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
15
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| Complexity |
271
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| Defined Atom Stereocenter Count |
0
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| SMILES |
[K].S=C(OC1C2C3C(C(C2)C1)CCC3)S
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| InChi Key |
IGULCCCBGBDZKQ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C11H16OS2.K/c13-11(14)12-10-5-6-4-9(10)8-3-1-2-7(6)8;/h6-10H,1-5H2,(H,13,14);/q;+1/p-1
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| Chemical Name |
potassium;8-tricyclo[5.2.1.02,6]decanyloxymethanedithioate
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| Synonyms |
D609D-609 D609
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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 : ~100 mg/mL (~375.29 mM)
H2O : ~2 mg/mL (~7.51 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (11.26 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 30.0 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: ≥ 3 mg/mL (11.26 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 30.0 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: ≥ 3 mg/mL (11.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 25 mg/mL (93.82 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.7529 mL | 18.7645 mL | 37.5291 mL | |
| 5 mM | 0.7506 mL | 3.7529 mL | 7.5058 mL | |
| 10 mM | 0.3753 mL | 1.8765 mL | 3.7529 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00669734 | ACTIVE, NOT RECRUITING | Biological: Falimarev Biological: Inalimarev Other: Laboratory Biomarker Analysis Biological: Sargramostim |
Locally Advanced Pancreatic Adenocarcinoma Pancreatic Acinar Cell Carcinoma Pancreatic Ductal Adenocarcinoma Stage III Pancreatic Cancer AJCC v6 and v7 Stage IV Pancreatic Cancer AJCC v6 and v7 |
National Cancer Institute (NCI) | 2010-02-01 | Phase 1 |
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