| Size | Price | Stock | Qty |
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| 5mg |
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| Targets |
The primary target of sAJM589 is the Myc protein, a transcription factor that regulates the expression of numerous genes involved in cell proliferation, growth, and metabolism. sAJM589 specifically disrupts the formation of Myc-Max heterodimers, which are essential for Myc transcriptional activity. By interfering with this protein-protein interaction, the compound prevents Myc from binding to its DNA recognition sites and activating target gene expression. The Myc-Max heterodimer is a well-established oncogenic driver in many human cancers, making it an attractive therapeutic target. sAJM589's mechanism of action is protein-dependent.
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| ln Vitro |
sAJM589 has an IC50 of 1.8 μM and efficiently lowers Myc levels by disrupting the Myc-Max heterodimer in a protein-dependent way [1]. sAJM589 prevents adherent, trouble-free Raji cell development as well as the multiplication of many Myc-dependent cells [1].
In vitro studies have demonstrated that sAJM589 effectively disrupts the Myc-Max heterodimer with an IC₅0 of 1.8 microM. It reduces Myc protein levels in a dose-dependent manner in various cancer cell lines. sAJM589 prevents the proliferation of adherent and non-adherent Myc-dependent cells, including Raji cells. The compound induces apoptosis in cancer cells by inhibiting Myc-mediated transcription of survival and proliferation genes. Its anti-proliferative and pro-apoptotic effects have been demonstrated in multiple Myc-dependent cancer cell lines, highlighting its potential as an anticancer agent. |
| ln Vivo |
In vivo studies of sAJM589 are primarily focused on its antitumor activity in animal models of Myc-driven cancers. As a Myc inhibitor that disrupts Myc-Max heterodimerization, sAJM589 is expected to reduce tumor growth in xenograft models. The compound's ability to induce apoptosis and inhibit proliferation in cancer cells suggests it could be effective in vivo against tumors that are dependent on Myc for survival and growth. Further studies are needed to evaluate its pharmacokinetic properties, bioavailability, and efficacy in various animal models of cancer. sAJM589 represents a promising approach for targeting the Myc oncogene, which has long been considered an "undruggable" target.
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| Enzyme Assay |
For in vitro enzyme/receptor binding assays, sAJM589 can be evaluated using biochemical assays that measure the disruption of Myc-Max heterodimer formation. These assays typically involve recombinant Myc and Max proteins and utilize techniques such as fluorescence polarization (FP), AlphaScreen, or ELISA to quantify the interaction. The compound is incubated with the proteins at various concentrations, and the IC₅0 for inhibiting heterodimer formation is determined. Surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC) can be used to measure the binding affinity and thermodynamics of the interaction. Standard assay conditions include physiological buffer systems with appropriate pH and ionic strength.
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| Cell Assay |
For in vitro cellular experiments, sAJM589 is typically tested in Myc-dependent cancer cell lines such as Raji (Burkitt's lymphoma) or other cell lines with elevated Myc expression. Cells are cultured in appropriate media and treated with various concentrations of the compound (typically ranging from nanomolar to micromolar) for defined periods. Cell viability and proliferation are assessed using MTT, CellTiter-Glo, or colony formation assays. Apoptosis is evaluated using Annexin V staining, caspase activity assays, or TUNEL staining. Myc protein levels are measured by Western blotting or immunofluorescence. Gene expression changes are analyzed by qPCR or RNA sequencing to confirm target engagement and downstream effects.
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| Animal Protocol |
For in vivo animal experiments, sAJM589 can be administered to tumor-bearing mice via various routes including oral gavage, intravenous injection, or intraperitoneal injection. Xenograft models using Myc-dependent human cancer cell lines in immunodeficient mice are commonly used to evaluate antitumor efficacy. Typical dosing regimens may range from 1 to 100 mg/kg administered daily or intermittently. Tumor volume is measured regularly using calipers, and tumor growth inhibition is calculated. Body weight and overall health are monitored as indicators of tolerability. At study termination, tumors and tissues are collected for analysis of Myc protein levels, apoptosis markers, and pharmacokinetic parameters.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of sAJM589 have not been extensively characterized in the public literature. As a small molecule with a molecular weight of 246.26 g/mol, it may have reasonable oral bioavailability and tissue distribution. The compound's lipophilicity and protein binding would influence its pharmacokinetic profile. Detailed parameters such as Cₘₐₓ, Tₘₐₓ, AUC, half-life, and clearance would need to be determined through comprehensive PK studies in relevant animal models. The compound's metabolism, potential for drug-drug interactions, and excretion pathways remain to be fully elucidated. Formulation development may be necessary for optimal in vivo administration.
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| Toxicity/Toxicokinetics |
Toxicological data for sAJM589 are limited, as the compound is primarily a research tool. Preliminary studies suggest that sAJM589 is well-tolerated in cell-based assays at concentrations that are effective for inhibiting Myc-Max heterodimerization. However, comprehensive toxicology studies including acute and repeated-dose toxicity, genotoxicity, and cardiotoxicity assessments would be needed for further development. As an inhibitor of Myc, which is a critical regulator of normal cell proliferation, potential on-target toxicities in rapidly dividing normal tissues (such as bone marrow and intestinal epithelium) should be considered. Appropriate safety precautions should be taken when handling this compound.
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| References | |
| Additional Infomation |
sAJM589 is a research compound primarily used in cancer research to study Myc biology and validate Myc as a therapeutic target. No clinical trials or regulatory approvals have been reported for this compound as a therapeutic agent. It is available from various chemical suppliers for research purposes only. sAJM589 represents a valuable tool for investigating the role of Myc in cancer and for developing strategies to target this important oncogene. Its ability to disrupt Myc-Max heterodimerization provides a chemical probe for studying Myc-dependent cellular processes and for evaluating the therapeutic potential of Myc inhibition.
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| Molecular Formula |
C16H10N2O
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| Molecular Weight |
246.2634
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| Exact Mass |
246.079
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| CAS # |
2089-82-9
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| PubChem CID |
135480579
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| Appearance |
Yellow to orange solid powder
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| LogP |
3.641
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
19
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| Complexity |
335
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C(=CC3=NC4=CC=CC=C4N=C23)O
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| InChi Key |
WZBDRAAGHRCRKM-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H10N2O/c19-15-9-14-16(11-6-2-1-5-10(11)15)18-13-8-4-3-7-12(13)17-14/h1-9,19H
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| Chemical Name |
benzo[a]phenazin-5-ol
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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 : ~5 mg/mL (~20.30 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.0607 mL | 20.3037 mL | 40.6075 mL | |
| 5 mM | 0.8121 mL | 4.0607 mL | 8.1215 mL | |
| 10 mM | 0.4061 mL | 2.0304 mL | 4.0607 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.
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