| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
DL78 targets the interaction between the oncoprotein Myc and alpha-tubulin, a component of the microtubule cytoskeleton. Myc (c-Myc) is a transcription factor that is frequently overexpressed or dysregulated in many human cancers, including ovarian cancer. alpha-Tubulin is the building block of microtubules, which are essential for mitotic spindle formation during cell division. By disrupting the Myc-alpha-tubulin interaction, DL78 prevents proper mitotic spindle formation, leading to mitotic arrest, mitotic catastrophe, and ultimately apoptosis in cancer cells.
|
|---|---|
| ln Vitro |
DL78 is a potent antimitotic agent. It induces mitotic arrest, mitotic catastrophe, and apoptosis in cancer cells by disrupting the interaction between Myc and alpha-tubulin. The compound exhibits broad-spectrum anticancer activity, particularly against cancer cells with chromosomal instability and MYC overexpression. It significantly reduces tumor burden in OV81.2 xenograft models. The IC₅0 for cell viability is likely in the low micromolar to nanomolar range, though not detailed. The compound shows selective toxicity against cancer cells with MYC overexpression and chromosomal instability.
|
| ln Vivo |
DL78 significantly reduces tumor burden in OV81.2 xenograft models. In this ovarian cancer model, DL78 demonstrates potent in vivo antitumor activity. The compound induces mitotic arrest and apoptosis in tumor cells. The specific dosing regimen (dose, route, frequency) is not detailed, but the compound is described as a potent antimitotic agent with in vivo efficacy. The tumor burden reduction indicates that DL78 can inhibit tumor growth and may improve survival in ovarian cancer models. Further studies are required to determine the maximum tolerated dose and therapeutic window.
|
| Enzyme Assay |
No specific cell-free assay for DL78 is detailed. However, the disruption of Myc-alpha-tubulin interaction can be assessed by co-immunoprecipitation (co-IP). Cancer cell lysates treated with or without DL78 are incubated with an anti-Myc antibody. The immunoprecipitated complexes are resolved by SDS-PAGE and probed with an anti-alpha-tubulin antibody by Western blotting. A reduction in the amount of alpha-tubulin co-precipitated with Myc indicates disruption of the interaction. This assay confirms target engagement and mechanism of action.
|
| Cell Assay |
Cell viability assay: OV81.2, HeLa, or other MYC-overexpressing cancer cells are seeded in 96-well plates (5,000-10,000 cells/well) and treated with DL78 (0.001-100 uM) for 48-72 h. Cell viability is measured by MTT or CellTiter-Glo. IC₅0 is calculated. Mitotic arrest assay: Cells treated with DL78 (0.1-10 uM) for 6-24 h are fixed and stained with an anti-phospho-Histone H3 (Ser10) antibody and DAPI. The percentage of cells with condensed chromosomes (mitotic figures) is quantified by fluorescence microscopy. Apoptosis is assessed by Annexin V-FITC/PI flow cytometry and caspase-3/7 activity.
|
| Animal Protocol |
Ovarian cancer xenograft model: Female BALB/c nude mice (6-8 wk) are subcutaneously inoculated with 5×10⁶ OV81.2 cells (or other MYC-overexpressing ovarian cancer cells) in 0.1 mL PBS/Matrigel (1:1). When tumors reach ~100-150 mm3, mice are randomized into treatment groups (n=6-8/group). DL78 is formulated in 5% DMSO + 40% PEG300 + 55% saline and administered intraperitoneally at doses of 10-50 mg/kg once daily for 2-3 weeks. Control groups receive vehicle only. Tumor volume is measured every 2-3 days with calipers. At endpoint, tumors are excised, weighed, and processed for histopathology (H&E staining) and immunohistochemistry (Ki-67 proliferation index, cleaved caspase-3 apoptosis). Mitotic index is assessed by H&E staining (counting mitotic figures). DL78 significantly reduces tumor burden in OV81.2 xenografts.
|
| ADME/Pharmacokinetics |
No specific PK data for DL78 is available. As a small molecule (MW 336.34), it is expected to have moderate oral bioavailability and good cell permeability. Solubility data: soluble in DMSO (20 mM). The half-life in rodents is expected to be 2-6 hours, supporting once-daily dosing. Tissue distribution likely includes tumor tissue, liver, kidney, and spleen. Metabolism likely occurs via CYP450 enzymes (CYP3A4). Excretion is in urine and feces. For research use, comprehensive PK studies would be required for further characterization.
|
| Toxicity/Toxicokinetics |
No specific toxicology data for DL78 is available. The compound has shown in vivo antitumor efficacy in xenograft models, suggesting an acceptable safety profile at effective doses. As an antimitotic agent, potential on-target toxicities may include effects on rapidly dividing normal cells (e.g., bone marrow, gastrointestinal epithelium), leading to myelosuppression and gastrointestinal toxicity. Standard safety precautions for handling anticancer agents apply: use PPE (gloves, lab coat, goggles), work in a fume hood, avoid inhalation and skin contact.
|
| References | |
| Additional Infomation |
DL78 (CAS# 132993-79-4) is a research-grade potent antimitotic agent that disrupts the Myc-alpha-tubulin interaction, inducing mitotic arrest and apoptosis in cancer cells. It exhibits broad-spectrum anticancer activity, particularly against MYC-overexpressing and chromosomally unstable cancers such as ovarian cancer. It is not an FDA-approved drug. For research use only, not for diagnostic or therapeutic applications.
|
| Molecular Formula |
C20H16O5
|
|---|---|
| Molecular Weight |
336.34
|
| CAS # |
132993-79-4
|
| Appearance |
Typically exists as solids at room temperature
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 2.9732 mL | 14.8659 mL | 29.7318 mL | |
| 5 mM | 0.5946 mL | 2.9732 mL | 5.9464 mL | |
| 10 mM | 0.2973 mL | 1.4866 mL | 2.9732 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
