| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 100mg | |||
| Other Sizes |
| Targets |
AS101 targets multiple pathways involved in immune regulation. It inhibits IL-1β and IL-1beta converting enzyme. It abolishes phosphorylation of STAT3 by inhibiting IL-10. It is a potent inducer of IL-1 and IL-6. By modulating these cytokines and signaling pathways, AS101 exerts immunomodulatory effects.
|
|---|---|
| ln Vitro |
For a whole day, ossirene (AS101; 1 μg/mL) virtually eliminated pStat3 expression. Ossirene can decrease Bcl-2 expression by blocking IL-10, which in turn inhibits Stat3 activation [2]. In RPE, AS101 (0.5, 5 mg/mL; 24 hours) dose-dependently suppresses the mRNA expression of inflammatory mediators generated by IL-1β. In RPE cells, AS101 suppresses IL-1β-induced mRNA expression and IL-6 and IL-8 protein synthesis. The phosphorylation of the p65 component of the NFκB complex, which is triggered by IL-1β, is inhibited by AS101 (5 mg/mL; 1 hour) [1]. Ossirene (0.1, 0.5, 1, 2.5 μg/mL) dramatically inhibits the growth of human glioblastoma multiforme (GBM) cells, gastric adenocarcinoma, and B16 melanoma [2]. In an IL-10-dependent way, AS101 (0.5 μg/mL) sensitizes GBM tumor cells to paclitaxel during a 24-hour period [2].
In vitro, AS101 is a potent immunomodulator. It inhibits IL-1β and IL-1beta converting enzyme. It abolishes phosphorylation of STAT3 by inhibiting IL-10. It induces IL-1 and IL-6. These in vitro activities confirm its profile as a potent immunomodulatory agent with diverse effects on cytokine production and signaling. |
| ln Vivo |
Ossirene (AS101; 0.5 mg/kg/day; i.p.; 25 days) sensitizes GBM tumors to paclitaxel by suppressing IL-10, hence enhancing survival [2].
In vivo, AS101 is a potent immunomodulator. It has immuno-modulating, antiviral, and hair growth-promoting activities. However, specific details of in vivo efficacy studies are not extensively detailed in the available literature. The compound is a research tool for studying immunomodulation and inflammation. |
| Enzyme Assay |
The in vitro enzyme/receptor binding assays for AS101 measure its ability to inhibit IL-1beta converting enzyme (caspase-1) activity. These cell-free assays use purified caspase-1 and a substrate. The compound's inhibitory potency is determined by measuring the reduction in enzyme activity. Its effects on cytokine production and STAT3 phosphorylation are assessed in cellular systems.
|
| Cell Assay |
Western Blot Analysis[2]
Cell Types: B16 Melanoma Cells Tested Concentrations: 1 μg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Expression of pStat3 was almost completely eliminated. RT-PCR[1] Cell Types: ARPE19 Cell Tested Concentrations: 0.5, 5 mg/mL Incubation Duration: 24 hrs (hours) Experimental Results: Inhibited IL-1β-induced expression of inflammatory mediator mRNA in RPE in a dose-dependent manner. In vitro cellular assays for AS101 assess its effects on cytokine production and signaling in immune cells. Cells are treated with AS101, and the production of IL-1β, IL-6, and IL-10 is measured. STAT3 phosphorylation is assessed by Western blot. These assays demonstrate the compound's immunomodulatory effects in a relevant cellular context. |
| Animal Protocol |
Animal/Disease Models: SCID (severe combined immunodeficient) mouse with GBM cells [2]
Doses: 0.5 mg/kg Route of Administration: IP; daily; 25 days Experimental Results: The survival rate of GBM tumor mice was Dramatically improved. In vivo animal studies for AS101 have been conducted to assess its immunomodulatory, antiviral, and hair growth-promoting activities. However, specific details of these studies are not extensively detailed in the available literature. The compound is a research tool for studying immunomodulation and inflammation. |
| ADME/Pharmacokinetics |
Specific pharmacokinetic data for AS101 are not extensively detailed in the available literature. As a tellurium compound, its pharmacokinetic properties would be important for its in vivo efficacy. However, specific parameters such as oral bioavailability, half-life, and distribution are not provided. The compound is primarily used in research settings.
|
| Toxicity/Toxicokinetics |
AS101 is a synthetic non-toxic tellurium derivative, structurally similar to cisplatin. It is a potent in vitro and in vivo immunomodulator. It inhibits IL-1β and IL-1beta converting enzyme. It has immuno-modulating, antiviral, and hair growth-promoting activities. It is a research compound for studying immunomodulation and is not approved for clinical use.
|
| References |
|
| Molecular Formula |
C2H8CL3NO2TE
|
|---|---|
| Molecular Weight |
312.049416542053
|
| Exact Mass |
312.868
|
| CAS # |
106566-58-9
|
| PubChem CID |
155561795
|
| Appearance |
White to off-white solid powder
|
| Density |
1.097g/cm3
|
| Boiling Point |
197.5ºC at 760mmHg
|
| Flash Point |
108.2ºC
|
| LogP |
2.012
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
3
|
| Rotatable Bond Count |
0
|
| Heavy Atom Count |
9
|
| Complexity |
97.6
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1CO[Te](O1)(Cl)(Cl)Cl.N
|
| InChi Key |
JKJLHRGACLEQMQ-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C2H4Cl3O2Te.H3N/c3-8(4,5)6-1-2-7-8;/h1-2H2;1H3
|
| 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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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 : ~12.5 mg/mL (~40.06 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 1.25 mg/mL (4.01 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: 1.25 mg/mL (4.01 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 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: ≥ 1.25 mg/mL (4.01 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 | 3.2046 mL | 16.0231 mL | 32.0461 mL | |
| 5 mM | 0.6409 mL | 3.2046 mL | 6.4092 mL | |
| 10 mM | 0.3205 mL | 1.6023 mL | 3.2046 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 |
| NCT00926354 | Terminated | Drug: AS101 | Chemotherapy Induced Thrombocytopenia | BioMAS Ltd | 2009-08 | Phase 2 |
| NCT01010373 | Suspended | Drug: AS101 | Acute Myeloid Leukemia Myelodysplastic Syndrome |
BioMAS Ltd | 2015-01 | Phase 2 |
| NCT00788424 | Withdrawn | Drug: AS101 Cream | Mild to Moderate Psoriasis | BioMAS Ltd | 2008-11 | Phase 2 |
| NCT01555112 | Completed | Drug: Topical AS101 | Condyloma Acuminata Wart; External Genital Organs |
BioMAS Ltd | 2012-03 | Phase 1 Phase 2 |
| NCT03216538 | Completed | Drug: AS101 1% oral solution Drug: Placebo |
Neovascular Age-related Macular Degeneration | Feramda | 2018-10-08 | Phase 1 Phase 2 |
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
