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5mg |
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10mg |
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Other Sizes |
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Lanreotide TFA (BIM-23014; Ipstyl; BIM 23014; Somatulin), the trifluoroacetate salt of lanreotide and synthetic somatostatin analogue, is an approved peptide based anticancer medication used in the management of acromegaly and symptoms caused by neuroendocrine tumors, most notably carcinoid syndrome.
ln Vitro |
Lanreotide (BIM 23014) (100 nM; 0-48 h) increases the apoptosis caused by radiation [1]. The development of GH3 cell colonies was decreased by lanreotide in a dose-dependent manner. Cell survival rates were 75%, 56%, 39%, and 27% at lanreotide doses of 1, 10, 100, and 1000 nM, respectively. 57 nM is the IC50[1]. In vitro, lanreotide suppresses the growth and hormone release of pituitary adenoma cells that secrete growth hormone [2].
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ln Vivo |
Tumor development is inhibited by lanreotide acetate (2.5–10 mg/kg; subcutaneous injection; once daily for 5 days) [1].
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Cell Assay |
Apoptosis analysis[1]
Cell Types: GH3 Tested Concentrations: 100 nM Incubation Duration: 48 hrs (hours), 24 hrs (hours) or immediately before irradiation (0 hrs (hours)) Experimental Results: Increased proportion of apoptotic sub-G1 compared to irradiation alone. |
Animal Protocol |
Animal/Disease Models: Male nude mouse, 8 weeks old, weighing 20-25 g (GH3 tumor-bearing nude mouse) [1]
Doses: 2.5, 5, 10 mg/kg Route of Administration: subcutaneous injection; one time/day for 5 days. Experimental Results: Produce tumor growth inhibition effect. |
References |
[1]. Ning S, et al. Lanreotide promotes apoptosis and is not radioprotective in GH3 cells.Endocr Relat Cancer. 2009 Sep;16(3):1045-55.
[2]. Florio T, et al. Characterization of the intracellular mechanisms mediating somatostatin and lanreotide inhibition of DNA synthesis and growth hormone release from dispersed human GH-secreting pituitary adenoma cells in vitro.Clin Endocrinol (Oxf). 2003 Jul;59(1):115-28. |
Molecular Formula |
C56H73N11O12S2
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Molecular Weight |
1156.37533068657
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CAS # |
2378114-72-6
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Related CAS # |
Lanreotide;108736-35-2;Lanreotide diTFA;1024499-83-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
S1C[C@@H](C(N[C@H](C(N)=O)[C@@H](C)O)=O)NC([C@H](C(C)C)NC([C@H](CCCCN)NC([C@@H](CC2=CNC3C=CC=CC2=3)NC([C@H](CC2C=CC(=CC=2)O)NC([C@H](CS1)NC([C@@H](CC1C=CC2C=CC=CC=2C=1)N)=O)=O)=O)=O)=O)=O.OC(C)=O
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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 (~86.48 mM)
H2O : ~25 mg/mL (~21.62 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.16 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 25.0 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: ≥ 2.5 mg/mL (2.16 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 25.0 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: ≥ 2.5 mg/mL (2.16 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 | 0.8648 mL | 4.3238 mL | 8.6477 mL | |
5 mM | 0.1730 mL | 0.8648 mL | 1.7295 mL | |
10 mM | 0.0865 mL | 0.4324 mL | 0.8648 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.