Physicochemical Properties
| Molecular Formula | C57H80CLN13O12S2 |
| Molecular Weight | 1238.91 |
| Appearance | White to off-white solid powder |
| 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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition | Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs) |
Biological Activity
| Targets | SSTR2 SSTR5 |
| ln Vitro | PRL secretion is often modestly stimulated by BIM-23190[1]. |
| ln Vivo | BIM-23190 has notable anti-tumor (C6 glioma) efficacy when given twice daily at a dose of 50 μg/mouse[2]. |
| Animal Protocol |
Animal/Disease Models: Male athymic nude (nu/nu) mice, 5-6 wk old (C6 glioma)[ 2]. Doses: 50 μg/mouse. Route of Administration: Injected twice a day for 19 days. Experimental Results: Dramatically decreased the tumor growth rate. |
| References |
[1]. Somatostatin receptor (SSTR) subtype-selective analogues differentially suppress in vitro growth hormone and prolactin in human pituitary adenomas. Novel potential therapy for functional pituitary tumors. J Clin Invest. 1997 Nov 1;100(9):2386-92. [2]. Differential efficacy of SSTR1, -2, and -5 agonists in the inhibition of C6 glioma growth in nude mice. Am J Physiol Endocrinol Metab. 2009 Nov;297(5):E1078-88. [3]. Novel somatostatin analogs for the treatment of acromegaly and cancer exhibit improved in vivo stability and distribution. J Pharmacol Exp Ther. 1998 Apr;285(1):95-104. |
Solubility Data
| Solubility (In Vitro) |
DMSO :~100 mg/mL (~80.72 mM) H2O :~100 mg/mL (~80.72 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.02 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 (2.02 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. Solubility in Formulation 3: ≥ 2.5 mg/mL (2.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. Solubility in Formulation 4: 50 mg/mL (40.36 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.8072 mL | 4.0358 mL | 8.0716 mL | |
| 5 mM | 0.1614 mL | 0.8072 mL | 1.6143 mL | |
| 10 mM | 0.0807 mL | 0.4036 mL | 0.8072 mL |