| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
SSTR2 SSTR5
BIM-23190 hydrochloride selectively targets somatostatin receptor subtypes 2 (SSTR2) and 5 (SSTR5). These are G protein-coupled receptors that are widely expressed in various tissues, including the pituitary, pancreas, and brain, and are often overexpressed in neuroendocrine tumors. Activation of SSTR2 and SSTR5 leads to inhibition of hormone secretion and cell proliferation. The selectivity for SSTR2 over SSTR5 is approximately 30-fold, with Ki values of 0.34 nM and 11.1 nM, respectively. |
|---|---|
| ln Vitro |
PRL secretion is often modestly stimulated by BIM-23190[1].
In vitro, BIM-23190 tends to mildly stimulate PRL (prolactin) secretion in certain cell models. This effect is likely mediated through somatostatin receptor activation. While the compound is a selective SSTR2/SSTR5 agonist, detailed cellular EC50 values for growth inhibition are not extensively provided in the available literature, but it is known to influence cell signaling pathways associated with somatostatin receptor activation. It exhibits antiproliferative effects in various cancer cell lines. |
| ln Vivo |
BIM-23190 has notable anti-tumor (C6 glioma) efficacy when given twice daily at a dose of 50 μg/mouse[2].
In vivo, BIM-23190 exhibits significant anti-tumor activity in a C6 glioma xenograft mouse model. In the study, male athymic nude mice bearing C6 glioma tumors were injected with BIM-23190 at a dose of 50 microg/mouse, twice per day for 19 days. The treatment significantly reduced the tumor growth rate compared to controls. This demonstrates the potential of BIM-23190 as an anti-cancer research agent for tumors expressing SSTR2 and SSTR5. |
| Enzyme Assay |
The binding affinity of BIM-23190 for somatostatin receptors is determined using radioligand binding assays on membrane preparations from cells expressing recombinant human SSTR2 or SSTR5. Various concentrations of BIM-23190 are incubated with a labeled somatostatin analog (e.g., 125I-Tyr11-SRIF-14) in a binding buffer. After incubation, bound and free radioligands are separated by filtration, and radioactivity is measured. Ki values are calculated from competition curves.
|
| Cell Assay |
Cellular assays for BIM-23190 are conducted using somatostatin receptor-expressing tumor cell lines, such as C6 glioma cells or neuroendocrine tumor cells. Cells are treated with varying concentrations of BIM-23190 for 24-72 hours. Cell proliferation is measured using standard viability assays like CCK-8, MTT, or BrdU incorporation assays. Additionally, hormone secretion (e.g., growth hormone, prolactin) can be measured in culture supernatants by ELISA to assess functional receptor activation.
|
| 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. In vivo tumor efficacy studies are performed using xenograft mouse models. For the C6 glioma model, 5-6 week old male athymic nude mice are subcutaneously injected with C6 glioma cells. When tumors reach a certain size, BIM-23190 hydrochloride is administered by subcutaneous injection at 50 microg/mouse, twice daily for 19 days. Tumor volumes are measured every few days using calipers, and tumor growth curves are generated. At study termination, tumors are excised and weighed. |
| ADME/Pharmacokinetics |
Pharmacokinetic data for BIM-23190 hydrochloride are not extensively detailed in product literature. As a peptide somatostatin analog, it is likely to have a relatively short half-life requiring frequent administration (twice daily in animal studies). Comprehensive ADME parameters would need to be determined experimentally, including bioavailability, half-life, and tissue distribution. The compound is typically administered by injection rather than orally due to peptide stability issues.
|
| Toxicity/Toxicokinetics |
Comprehensive toxicological data for BIM-23190 hydrochloride are not extensively reported in standard product literature. In the reported in vivo study at 50 microg/mouse twice daily for 19 days, no overt toxicity or significant adverse effects were described. Standard preclinical safety assessments including acute and repeated-dose toxicity, genotoxicity, and safety pharmacology would be required for therapeutic development. For research use, standard peptide handling precautions apply.
|
| References |
|
| Additional Infomation |
BIM-23190 hydrochloride has a molecular weight of 1238.91 and the molecular formula C57H80ClN13O12S2. The peptide sequence contains D-Phe and D-Trp residues, typical of somatostatin analogs. The compound is a somatostatin analog developed for research on acromegaly and neuroendocrine tumors. It is a selective agonist for SSTR2 and SSTR5. No clinical development or regulatory approval has been reported in standard product literature. It is for research use only.
|
| 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)
|
| 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. View More
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. 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. |
| 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 |
*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
