| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
The primary target of ETN029 is DLL3 (Delta‑like protein 3). ETN029 functions as a ligand that binds to DLL3, a protein expressed on the surface of certain cancer cells, particularly in small cell lung cancer (SCLC), neuroendocrine prostate cancer (NEPC), and metastatic melanoma. By binding to DLL3, the compound can deliver a conjugated therapeutic payload, such as a radioactive atom, specifically to cancer cells.
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| ln Vitro |
In vitro, ETN029 labeled with 22⁵Ac exhibits dose‑dependent cytotoxicity against small cell lung cancer (SCLC), neuroendocrine prostate cancer (NEPC), and metastatic melanoma cells, and promotes H2AX phosphorylation. The cytotoxicity is due to DNA damage induced by the alpha‑emitter 22⁵Ac. The EC₅0 (half‑maximal effective concentration) for killing SCLC cells is in the nanomolar range.
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| ln Vivo |
In vivo, ETN029 labeled with ¹⁷⁷Lu shows rapid uptake, persistent tumor retention, and a favorable tumor-to-kidney ratio. This makes it a promising candidate for imaging and targeted radionuclide therapy of cancers such as SCLC and NEPC. The compound effectively accumulates in tumors and remains there while clearing from normal tissues, especially the kidneys, thereby enhancing therapeutic efficacy and reducing toxicity.
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| Enzyme Assay |
Non-cell-based (cell-free) experiments for ETN029 focus on its labeling efficiency with radioisotopes. A standard protocol for radiolabeling with ¹⁷⁷Lu involves mixing ETN029 (typically 1-100 ug) with ¹⁷⁷LuCl3 in an ammonium acetate buffer (e.g., 0.1 M, pH 5.5) at 37degC for 30-60 minutes. The radiolabeling yield is measured by instant thin-layer chromatography (ITLC) using a gamma counter to detect the radioactive signal. The stability of the radiolabeled compound in serum is assessed by incubating it with human serum at 37degC for up to 72 hours, followed by ITLC analysis to measure any dissociation of the radioisotope. The binding affinity (KD) of ETN029 to DLL3 can be measured by surface plasmon resonance (SPR) using immobilized recombinant DLL3 protein.
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| Cell Assay |
Cell-based experiments for ETN029 are designed to evaluate its radiopharmaceutical properties. SCLC cells (e.g., NCI‑H69, DMS 53) are seeded in 96‑well plates and treated with increasing concentrations of 22⁵Ac‑ or ¹⁷⁷Lu‑labeled ETN029 (0.001-100 nM). After 48-72 hours, cell viability is measured using an MTT or CellTiter‑Glo assay. The IC₅0 (half‑maximal inhibitory concentration) is calculated. DNA damage is assessed by immunocytochemistry: cells are fixed and stained with an anti‑gammaH2AX antibody (phosphorylated H2AX is a marker of DNA double‑strand breaks). The number of gammaH2AX foci per nucleus is counted using a fluorescence microscope. Internalization studies: cells are incubated with radiolabeled ETN029 at 4degC (surface binding) and 37degC (internalization), and the fraction of cell‑associated radioactivity that is resistant to acid wash is determined using a gamma counter.
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| Animal Protocol |
In vivo animal experiments for ETN029 are conducted in mouse models of SCLC. Nude mice are xenografted subcutaneously or orthotopically with SCLC cells (e.g., NCI‑H69). When tumors reach a certain size, the mice are injected intravenously with ¹⁷⁷Lu‑ETN029 (e.g., 1-10 MBq per mouse). Biodistribution is evaluated by sacrificing groups of mice at various time points (e.g., 1, 4, 24, 48, 96 h) and dissecting the tumors and major organs (liver, kidneys, spleen, lungs, blood). The radioactivity in each tissue is measured by a gamma counter, and the percentage of injected dose per gram of tissue (%ID/g) is calculated. For therapy studies, mice are injected with a therapeutic dose of 22⁵Ac‑ETN029, and tumor size is measured by calipers twice a week. Survival is monitored, and the Kaplan‑Meier curve is plotted.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for ETN029 are derived from the biodistribution studies of its radiolabeled forms. The unlabeled compound has a molecular weight of 2142.45 g/mol. After injection, the radiolabeled compound shows rapid uptake and persistent retention in tumors, with a favorable tumor-to-kidney ratio. It is suitable for imaging SCLC and NEPC. The compound is stored as a powder at -20degC (stable for up to 3 years) or in a solvent at -80degC.
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| Toxicity/Toxicokinetics |
The toxicity of ETN029 is related to its delivery of a cytotoxic radionuclide. The unlabeled compound is not inherently toxic; toxicity arises from the DNA damage induced by the ionizing radiation of isotopes like 22⁵Ac and ¹⁷⁷Lu. This damage is specific to cells expressing the DLL3 target. As a research chemical, standard safety precautions for handling radioactive materials apply. The compound may be harmful if swallowed, inhaled, or absorbed through the skin. It may cause skin and eye irritation. Radiological safety protocols must be followed when handling the labeled compound.
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| References |
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| Additional Infomation |
Additional information: The compound has a molecular weight of 2142.45 g/mol and a purity of 99.91%. The CAS number is 3066864-32-9. It is also known as a DLL3 ligand. It is for research use only, not for human or veterinary use, and is not for diagnostic or therapeutic use in humans. It is a large peptide or peptide-like molecule (≥ 44 amino acids). Synonyms include ETN029, 3066864-32-9.
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| Molecular Formula |
C101H140N22O26S2
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| Molecular Weight |
2142.45
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| CAS # |
3066864-32-9
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| Appearance |
White to light yellow solid powder
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~46.68 mM; with sonication)
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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 | 0.4668 mL | 2.3338 mL | 4.6676 mL | |
| 5 mM | 0.0934 mL | 0.4668 mL | 0.9335 mL | |
| 10 mM | 0.0467 mL | 0.2334 mL | 0.4668 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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