| Size | Price | Stock | Qty |
|---|---|---|---|
| 250mg |
|
||
| 500mg |
|
||
| Other Sizes |
| Targets |
APC-100 targets the androgen receptor (AR) in target tissues. It binds to ARs, inhibiting androgen-induced receptor activation and facilitating the formation of inactive complexes that cannot be translocated 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.
|
|---|---|
| ln Vitro |
In vitro, APC-100 has potent androgen receptor signaling modulation and anti-cancer effects against prostate cancer/tumor cell lines. It inhibits the growth of both AR-dependent and AR-independent prostate tumor cells. It also functions as an antioxidant, reducing oxidative stress in cells. These activities support its potential as a chemopreventative and antineoplastic agent.
|
| ln Vivo |
In vivo, APC-100 has been used in trials studying the treatment of prostate cancer. By binding to ARs and inhibiting androgen-induced activation, it blocks the expression of androgen-responsive genes. A phase 1/2a dose-escalation study has been conducted in men with advanced prostate cancer. Its dual mechanism of action as an AR antagonist and antioxidant is key to its activity.
|
| Enzyme Assay |
The in vitro receptor binding assay for APC-100 typically involves radioligand displacement studies using the androgen receptor (AR). The compound's affinity for the AR is determined by measuring its ability to displace a specific radiolabeled ligand (e.g., [3H]-R1881) from the receptor. These cell-free assays provide a direct measure of the compound's binding affinity and confirm its role as an AR antagonist.
|
| Cell Assay |
In vitro cellular assays for APC-100 assess its functional activity as an AR antagonist. Prostate cancer cell lines are treated with APC-100, and the expression of androgen-responsive genes is measured. Its ability to inhibit androgen-induced cell proliferation is also assessed. These assays demonstrate the compound's functional antagonism at the AR in a relevant cellular context.
|
| Animal Protocol |
In vivo animal studies for APC-100 have been conducted in preclinical models of prostate cancer to evaluate its antitumor efficacy. However, specific details of these studies are not extensively detailed in the available literature. Clinical trials, including a multicenter phase 1/2a dose-escalation study, have been conducted in men with advanced prostate cancer.
|
| ADME/Pharmacokinetics |
APC-100 is an orally available compound. Its formulation as a small molecule allows for oral administration. The compound is a derivative of vitamin E, which is well-absorbed. Its pharmacokinetic properties support its use as an oral therapeutic agent. However, detailed parameters such as half-life and bioavailability are not extensively detailed in the available literature.
|
| Toxicity/Toxicokinetics |
Specific toxicity data for APC-100 are not extensively detailed in the available literature. As a vitamin E derivative and AR antagonist, its toxicity profile is likely related to its pharmacological activity. However, it has been investigated in clinical trials, indicating a manageable safety profile for further development. It is intended for research purposes only and is not approved for clinical use.
|
| 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.
APC-100 is a novel agent with a dual mechanism of action, functioning both as an antioxidant and as an AR antagonist. It has been investigated for the treatment of prostate cancer. It is a research compound and is not approved for clinical use. It is also known as 2,2,5,7,8-Pentamethyl-6-Chromanol (PMC). |
| 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 |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
