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Purity: ≥98%
4-IBP is a novel and selective σ1 (sigma1) agonist with high affinity for the σ1 receptor with Ki of 1.7 nM and a moderate affinity for the σ2 receptor (Ki = 25.2 nM). Although the molecular function of sigma receptors has not been fully defined and the natural ligand(s) is still not known, there is increasing evidence that these receptors and their ligands might play a significant role in cancer biology. 4-IBP has revealed weak antiproliferative effects on human U373-MG glioblastoma and C32 melanoma cells but induced marked concentration-dependent decreases in the growth of human A549 NSCLC and PC3 prostate cancer cells. The compound was also significantly antimigratory in all four cancer cell lines. This may result, at least in U373-MG cells, from modifications to the actin cytoskeleton. 4-IBP modified the sensitivity of U373-MG cells in vitro to proapoptotic lomustin and proautophagic temozolomide, and markedly decreased the expression of two proteins involved in drug resistance: glucosylceramide synthase and Rho guanine nucleotide dissociation inhibitor. In vivo, 4-IBP increased the antitumor effects of temozolomide and irinotecan in immunodeficient mice that were orthotopically grafted with invasive cancer cells.
| References |
Neoplasia.2007 May;9(5):358-69.
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| Molecular Formula |
C₁₉H₂₁IN₂O
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| Molecular Weight |
420.29
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| CAS # |
155798-08-6
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| SMILES |
O=C(NC1CCN(CC2=CC=CC=C2)CC1)C3=CC=C(I)C=C3
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.95 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 mg/mL (4.76 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 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3793 mL | 11.8965 mL | 23.7931 mL | |
| 5 mM | 0.4759 mL | 2.3793 mL | 4.7586 mL | |
| 10 mM | 0.2379 mL | 1.1897 mL | 2.3793 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.
Evaluation of the antiproliferative and antimotility activities of 4-IBP in cancer cells.Neoplasia.2007 May;9(5):358-69. |
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Immunofluorescence analyses in the investigation of the expression of Rho GDI (A–C) and GCS (D–F) in U373-MG GBM cells left untreated (A and D) or treated for 72 hours with 1 nM 4-IBP (B and E) and 10 nM 4-IBP (C and F).
Expression of the splice variants of σ1receptor mRNA (V1–V5) in four different human cancer cell lines, namely, melanoma (C32), refractory prostate (PC3), NSCLC (A549), and glioma (U373-MG) cells, as assessed by RT-PCR analyses.Neoplasia.2007 May;9(5):358-69. |
(A) The survival of mice orthotopically (brain) grafted with human U373-MG GBM cells after treatment with 4-IBP alone (red line) or combined with temozolomide (purple line), compared to temozolomide alone (green line) and controls (blue line). (B) The survival of mice orthotopically (lung) grafted with human A549 NSCLC cells after treatment with 4-IBP alone (red line) or combined with IRI (purple line), compared to IRI alone (green line) and controls (blue line).Neoplasia.2007 May;9(5):358-69. |
(A and B) Therapeutic combination of 4-IBP and cytotoxic agents [(A) lomustin and (B) temozolomide] in a scratch wound assay in which colonization by human U373-MG GBM cells of an artificially inflicted wound in a subconfluent cell population was followed over time.Neoplasia.2007 May;9(5):358-69. |
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(A) The detection and quantification of acidic vesicular organelles by acridine orange staining using flow cytometry in human U373-MG GBM cells treated for 72 hours with increasing concentrations of 4-IBP.Neoplasia.2007 May;9(5):358-69. |
Evaluation of 4-IBP - induced effects on U373-MG glioblastoma cells. (A) Illustration of the morphologic variables used to evaluate the roundness of a cell (level of sphericity, elongation, and morphologic pattern) and its spread (area).Neoplasia.2007 May;9(5):358-69. |
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