| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
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| 500mg |
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| Other Sizes |
| References | |
|---|---|
| Additional Infomation |
Chromanol is already being used in clinical trials for prostate cancer treatment. The androgen antagonist APC-100 is an orally administered vitamin E derivative and an androgen receptor (AR) antagonist with potential antioxidant, chemopreventive, and antitumor activities. APC-100 binds to AR in target tissues, thereby inhibiting androgen-induced receptor activation and promoting the formation of an inactive complex that cannot translocate to the nucleus. By inhibiting the formation of the complex between androgen-activated AR and the AP1 transcription factor JunD, the expression of androgen-responsive genes is blocked. One such gene is the spermine/spermine N1-acetyltransferase gene (SSAT), which is responsible for breaking down polyamines produced in large quantities by prostate epithelial cells into reactive oxygen species (ROS), which cause cell damage. APC-100 may ultimately lead to the inhibition of the growth of both AR-dependent and AR-dependent prostate tumor cells.
|
| Molecular Formula |
C14H20O2
|
|---|---|
| Molecular Weight |
220.3074
|
| Exact Mass |
220.146
|
| CAS # |
950-99-2
|
| PubChem CID |
99479
|
| Appearance |
White to off-white solid powder
|
| Density |
1.034g/cm3
|
| Boiling Point |
344.3ºC at 760 mmHg
|
| Melting Point |
89-91ºC(lit.)
|
| Flash Point |
146.1ºC
|
| Index of Refraction |
1.529
|
| LogP |
3.421
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
16
|
| Complexity |
262
|
| Defined Atom Stereocenter Count |
0
|
| InChi Key |
SEBPXHSZHLFWRL-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C14H20O2/c1-8-9(2)13-11(10(3)12(8)15)6-7-14(4,5)16-13/h15H,6-7H2,1-5H3
|
| Chemical Name |
2,2,5,7,8-pentamethyl-3,4-dihydrochromen-6-ol
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~1134.76 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (9.44 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 (9.44 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 (9.44 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 | 4.5391 mL | 22.6953 mL | 45.3906 mL | |
| 5 mM | 0.9078 mL | 4.5391 mL | 9.0781 mL | |
| 10 mM | 0.4539 mL | 2.2695 mL | 4.5391 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 |
| NCT01436214 | Unknown status | Drug: APC-100 | Prostate Cancer | Adamis Pharmaceuticals Corporation | 2011-08 | Phase 1 Phase 2 |
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