| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg | |||
| Other Sizes |
| Targets |
Bax-activator-106 targets the pro-apoptotic protein Bax. Bax is a member of the Bcl-2 family of proteins that plays a critical role in the intrinsic apoptosis pathway. Upon activation by apoptotic stimuli, Bax undergoes a conformational change, oligomerizes, and inserts into the mitochondrial outer membrane, leading to mitochondrial outer membrane permeabilization (MOMP), the release of cytochrome c, and activation of the caspase cascade. Bax-activator-106 is a specific Bax agonist that promotes Bax-dependent, but not Bak-dependent, apoptosis. By directly activating Bax, the compound triggers the mitochondrial apoptotic pathway, leading to cell death.
|
|---|---|
| ln Vitro |
Bax-dependent tumor cell death is induced in a dose-dependent manner by Bax activator-1 (20-80 μM; 48 hours) [1].
In vitro, Bax-activator-106 induces apoptosis in a dose-dependent manner. In studies using mouse Lewis lung cancer (LLC) cells, human non-small cell lung cancer A549 cells, and human pancreatic cancer Panc-1 cells, the compound at concentrations of 20-80 μM for 48 hours induced apoptosis in a dose-dependent manner. The compound's activity is specific to Bax, as it does not activate Bak. These in vitro studies confirm Bax-activator-106's mechanism of action as a Bax agonist and its potent pro-apoptotic activity in cancer cells. |
| ln Vivo |
In C57BL/6 female mice, the intraperitoneal injection of Bax activator-1 (40 mg/kg) suppresses the formation of lung tumors every day for 13 days [1].
In vivo, Bax-activator-106 has demonstrated antitumor activity as a single agent. In a study using C57BL/6 female mice bearing Lewis lung cancer tumor cells, daily intraperitoneal injection of Bax-activator-106 at 40 mg/kg for 13 days suppressed the formation of lung tumors. These findings provide evidence for the compound's in vivo efficacy as an anticancer agent. The compound's ability to induce Bax-dependent apoptosis makes it a promising candidate for cancer therapy. |
| Enzyme Assay |
In vitro assays for Bax-activator-106 measure its ability to induce apoptosis. In a typical assay, cancer cells are treated with the compound at various concentrations (e.g., 20-80 μM) for a defined period (e.g., 48 hours). Apoptosis is assessed using various methods, including Annexin V staining, caspase-3/7 activation assays, or TUNEL staining. The compound's ability to induce apoptosis in a dose-dependent manner is measured. These assays confirm the compound's pro-apoptotic activity.
|
| Cell Assay |
Apoptosis analysis [1]
Cell Types: Lewis lung cancer cells, human non-small cell lung cancer A549 cells, human pancreatic cancer Panc-1 cells Tested Concentrations: 20μM, 40μM, 60μM, 80μM Incubation Duration: 48 hrs (hours) Experimental Results: In a dose-dependent manner Induces apoptosis in mouse Lewis lung cancer (LLC), human non-small cell lung cancer A549 cells and PANC-1 human pancreatic cancer cells. In vitro cell-based assays for Bax-activator-106 are conducted using various cancer cell lines, including Lewis lung cancer cells, A549 lung cancer cells, and Panc-1 pancreatic cancer cells. Cells are treated with the compound at concentrations of 20, 40, 60, and 80 μM for 48 hours. Apoptosis is assessed using flow cytometry or other methods. The compound's ability to induce apoptosis in a dose-dependent manner is measured. These assays confirm the compound's activity as a Bax agonist and its potent pro-apoptotic effects in cancer cells. |
| Animal Protocol |
Animal/Disease Models: Eightweeks old C57BL/6 female mice (containing Lewis lung cancer tumor cells) [1]
Doses: 40 mg/kg Route of Administration: daily intraperitoneal (ip) injection for 13 days Experimental Results: demonstrated anti-tumor activity as a single agent agent. In vivo animal experiments for Bax-activator-106 have been conducted in a mouse model of lung cancer. In a typical study, eight-week-old C57BL/6 female mice containing Lewis lung cancer tumor cells are treated with the compound. Bax-activator-106 is administered by daily intraperitoneal (i.p.) injection at a dose of 40 mg/kg for 13 days. Tumor formation is monitored, and the compound's ability to suppress tumor growth is assessed. These studies provide evidence for the in vivo efficacy of Bax-activator-106 as an anticancer agent. |
| ADME/Pharmacokinetics |
Bax-activator-106 has a molecular weight of 488.62 g/mol and a molecular formula of C29H36N4O3. It has a CAS number of 1638526-94-9. It is a white to off-white solid powder with a purity of ≥98%. It has a logP of 3.6. For storage, it is recommended to keep the powder at -20°C. Detailed pharmacokinetic properties such as absorption, distribution, metabolism, and excretion (ADME) have not been extensively characterized. As a research compound, its stability is maintained by proper storage.
|
| Toxicity/Toxicokinetics |
Detailed toxicity data for Bax-activator-106 is not provided in standard product descriptions. In vivo studies have used the compound at a dose of 40 mg/kg in mice without reported overt toxicity. However, comprehensive toxicological studies have not been reported. As with all research chemicals, standard laboratory safety precautions should be followed when handling Bax-activator-106. Its use is limited to research applications and it is not intended for human or veterinary use.
|
| References | |
| Additional Infomation |
Bax-activator-106 is a research compound and is not approved for any clinical or therapeutic use. It is a specific Bax agonist that induces Bax-dependent tumor cell apoptosis. It has been shown to induce apoptosis in a dose-dependent manner in various cancer cell lines and to suppress tumor growth in a mouse model of lung cancer. Bax-activator-106 is a valuable research tool for studying apoptosis, the role of Bax in cancer, and for validating Bax as a therapeutic target. Its mechanism of action involves directly activating Bax to trigger the intrinsic apoptosis pathway.
|
| Molecular Formula |
C29H36N4O3
|
|---|---|
| Molecular Weight |
488.621147155762
|
| Exact Mass |
488.278
|
| CAS # |
1638526-94-9
|
| PubChem CID |
26230248
|
| Appearance |
White to off-white solid powder
|
| LogP |
3.6
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
36
|
| Complexity |
737
|
| Defined Atom Stereocenter Count |
1
|
| SMILES |
O[C@@H]1CCCN(C(C2C3CN(CC4C=CC(C)=C(C)C=4)CCC=3N(CC3C=CC=C(C=3)OC)N=2)=O)C1
|
| InChi Key |
OLNVSYZSZXRLCF-XMMPIXPASA-N
|
| InChi Code |
InChI=1S/C29H36N4O3/c1-20-9-10-23(14-21(20)2)16-31-13-11-27-26(19-31)28(29(35)32-12-5-7-24(34)18-32)30-33(27)17-22-6-4-8-25(15-22)36-3/h4,6,8-10,14-15,24,34H,5,7,11-13,16-19H2,1-3H3/t24-/m1/s1
|
| Chemical Name |
[5-[(3,4-dimethylphenyl)methyl]-1-[(3-methoxyphenyl)methyl]-6,7-dihydro-4H-pyrazolo[4,3-c]pyridin-3-yl]-[(3R)-3-hydroxypiperidin-1-yl]methanone
|
| Synonyms |
Bax-activator-106 Bax activator 106 Baxactivator106
|
| 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 (~511.65 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.26 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 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 (4.26 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 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 (4.26 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0466 mL | 10.2329 mL | 20.4658 mL | |
| 5 mM | 0.4093 mL | 2.0466 mL | 4.0932 mL | |
| 10 mM | 0.2047 mL | 1.0233 mL | 2.0466 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
