| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Somatostatin receptor (SSTR); specifically SSTR subtypes 1-5, with high affinity for SSTR2 and SSTR5; functions as an antagonist, blocking the binding of native somatostatin.
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| ln Vitro |
The TFA for 177Lu-DOTA-LM3 was tolerated. The body, kidneys, spleen, and metastases are the primary locations of 177Lu-DOTA-LM3 TFA, which raises the average absorbed dose to organs and tumors [2].
68Ga-DOTA-LM3 TFA exhibits good biodistribution, high tumor uptake, good tumor retention, and favorable safety profile; 177Lu-DOTA-LM3 TFA is used to study DOTATOC-negative liver metastases, including pancreatic NETs and extensive tumor thrombosis. |
| ln Vivo |
68Ga-DOTA-LM3 TFA shows high tumor uptake and good tumor retention in neuroendocrine tumor patients; 177Lu-DOTA-LM3 TFA has been evaluated in first-in-humans studies for peptide receptor radionuclide therapy (PRRT).
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| Enzyme Assay |
SSTR binding affinity assessed by competitive binding assays using radiolabeled SST analogs (e.g., 125I-Tyr3-octreotide) on SSTR-expressing cell membranes; IC50 values determined by displacement curves.
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| Cell Assay |
HEK293 cells or SSTR-expressing tumor cells (e.g., AR42J, BON-1) are incubated with 68Ga- or 177Lu-labeled DOTA-LM3 TFA (0.1-100 nM); cellular uptake and internalization are measured by gamma counting; saturation binding curves generated.
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| Animal Protocol |
Mice bearing SSTR-positive tumor xenografts (e.g., AR42J) receive 68Ga-DOTA-LM3 TFA (5-15 MBq, IV) for PET/CT imaging; for therapy, 177Lu-DOTA-LM3 TFA (10-30 MBq) is administered; tumor volume measured and dosimetry calculated.
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| ADME/Pharmacokinetics |
PK of radiolabeled DOTA-LM3 TFA: rapid clearance from blood; primarily cleared by kidneys; high tumor-to-background ratios achieved within 1-2 h post-injection; good tumor retention.
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| Toxicity/Toxicokinetics |
177Lu-DOTA-LM3 TFA was well-tolerated in a first-in-humans study; main accumulation observed in kidneys, spleen, and metastases; organ and tumor absorbed doses were acceptable; safety profile favorable.
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| References |
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| Additional Infomation |
177Lu-DOTA-LM3 TFA is under clinical investigation for PRRT in neuroendocrine neoplasms; not yet FDA/EMA approved; 68Ga-DOTA-LM3 TFA is under evaluation for diagnostic imaging; both in clinical trials.
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| Molecular Formula |
C71H94CLF3N16O21S2
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|---|---|
| Molecular Weight |
1664.18
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| Related CAS # |
DOTA-LM3;1192362-32-5
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| Appearance |
White to off-white 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) |
H2O :~100 mg/mL (~60.09 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 | 0.6009 mL | 3.0045 mL | 6.0090 mL | |
| 5 mM | 0.1202 mL | 0.6009 mL | 1.2018 mL | |
| 10 mM | 0.0601 mL | 0.3004 mL | 0.6009 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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