| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Targets |
BMS453 targets the retinoic acid receptor beta (RARβ), a nuclear receptor that regulates gene transcription. It acts as a selective agonist for RARβ, binding to the receptor and activating it. This leads to the transcription of RARβ target genes, many of which are involved in cell cycle regulation, differentiation, and apoptosis. BMS453 has been shown to have a higher affinity for RARβ than for RARα or RARγ.
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| ln Vitro |
Treatment with BMS453 (1 μM; 11 hours; 184 and HMEC cells) reduced the growth of normal breast cells without appreciably causing apoptosis [2]. BMS453 (1 μM; 5 days; 184 and HMEC cells) treatment induces G1 arrest, which prevents normal breast cell proliferation [2]. Treatment with 1 μM of BMS453 for 24–72 hours in 184 cells caused Rb hypophosphorylation and decreased CDK2 kinase activity. BMS453 does not alter CDK4 binding to p21, but it does raise levels of total p21 protein and CDK2 binding to p21 protein[2]. BMS453 primarily suppresses the development of breast cells by activating TGFβ [2].
In vitro, BMS453 has been shown to induce apoptosis and inhibit cell proliferation in various cancer cell lines. It activates RARβ-dependent gene transcription, leading to the expression of pro-apoptotic genes. BMS453 also inhibits the growth of cancer cells in a concentration-dependent manner. The compound has been shown to be effective against breast cancer cells, including those resistant to other retinoids. |
| ln Vivo |
In vivo, BMS453 has been studied in animal models of cancer, particularly in breast cancer. The compound has been shown to inhibit tumor growth in xenograft mouse models. BMS453 is typically administered orally or intraperitoneally. The compound's antitumor activity is associated with the induction of apoptosis and the inhibition of cell proliferation in the tumor tissue.
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| Enzyme Assay |
In vitro receptor binding assays for BMS453 typically involve measuring its affinity for RARβ, RARα, and RARγ using radioligand binding. The compound is incubated with nuclear extracts or recombinant receptors and a radiolabeled ligand such as [3H]retinoic acid. The concentration of BMS453 required to displace 50% of the radioligand (IC50) is determined, and the Ki value is calculated. The selectivity of BMS453 for RARβ over RARα and RARγ is assessed.
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| Cell Assay |
Cell proliferation assay [2]
Cell Types: Normal human breast epithelial cells (184 and HMEC) Tested Concentrations: 1 μM Incubation Duration: 11 hrs (hours) Experimental Results: 40% inhibition of 3H-thymidine uptake in normal breast cells (184 and HMEC). Cell cycle analysis [2] Cell Types: normal human mammary epithelial cells (184 and HMEC) Tested Concentrations: 1 μM Incubation Duration: 5 days Experimental Results: The proportion of cells in G0/G1 phase increased, and the proportion of cells in S phase diminished. Western Blot Analysis[2] Cell Types: 184 cells Tested Concentrations: 1 μM Incubation Duration: 24 hrs (hours), 48 hrs (hours), 72 hrs (hours) Experimental Results: Induced Rb hypophosphorylation and diminished CDK2 kinase activity. In vitro cell-based studies with BMS453 typically involve cultured cancer cell lines, such as breast cancer cells. Cells are treated with BMS453 at various concentrations for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. Apoptosis is evaluated by Annexin V/PI staining or by detecting caspase activity. RARβ-dependent gene transcription is assessed by measuring the expression of RARβ target genes using quantitative PCR. |
| Animal Protocol |
In vivo animal studies with BMS453 are typically conducted in xenograft mouse models of breast cancer. Tumor-bearing mice are treated with BMS453 via oral or intraperitoneal administration at various doses. Tumor growth is measured over time, and tumor growth inhibition is calculated. Tumor tissues are collected for histopathological analysis and for assessment of apoptosis and RARβ target gene expression. Pharmacokinetic studies are performed by measuring compound concentrations in plasma and tissues.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of BMS453 have been studied in preclinical settings. Following oral administration, the compound is absorbed from the gastrointestinal tract. BMS453 is metabolized in the liver. The elimination half-life is relatively short. Detailed PK parameters such as Cmax, Tmax, AUC, and half-life have been reported in the literature.
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| Toxicity/Toxicokinetics |
The toxicity profile of BMS453 has been evaluated in preclinical studies. The compound has been shown to have a relatively low toxicity in animal models at therapeutic doses. However, higher doses can cause adverse effects, including skin dryness, mucous membrane dryness, and hepatotoxicity. The compound is for research use only and is not approved for human therapeutic use.
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| References |
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| Additional Infomation |
BMS-453 belongs to the dihydronaphthalene class of compounds, with the structure 1,2-dihydronaphthalene, substituted at positions 1, 1, 4, and 6 with methyl, phenyl, and 2-(p-carboxyphenyl)vinyl groups, respectively (E-type isomers). It is a potent retinoic acid receptor γ (RARβ) agonist and also an antagonist of RARα and RARγ. It possesses dual functions as a retinoic acid receptor β agonist, retinoic acid receptor γ antagonist, retinoic acid receptor α antagonist, and teratogen. BMS-453 belongs to the dihydronaphthalene, benzoic acid, and stilbene classes of compounds.
BMS453 is a research compound with potent and selective agonist activity for the retinoic acid receptor beta (RARβ). It is used as a research tool to study RARβ signaling and its role in cancer and other diseases. BMS453 has been investigated for its potential therapeutic applications in breast cancer and other solid tumors. The compound is not an FDA-approved drug and is not commercially available as a pharmaceutical product. |
| Molecular Formula |
C27H24O2
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| Molecular Weight |
380.47826
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| Exact Mass |
380.178
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| CAS # |
166977-43-1
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| PubChem CID |
9875424
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| Appearance |
White to off-white solid powder
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| LogP |
6.668
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
29
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| Complexity |
629
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC1(CC=C(C2=C1C=CC(=C2)/C=C/C3=CC=C(C=C3)C(=O)O)C4=CC=CC=C4)C
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| InChi Key |
VUODRPPTYLBGFM-CMDGGOBGSA-N
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| InChi Code |
InChI=1S/C27H24O2/c1-27(2)17-16-23(21-6-4-3-5-7-21)24-18-20(12-15-25(24)27)9-8-19-10-13-22(14-11-19)26(28)29/h3-16,18H,17H2,1-2H3,(H,28,29)/b9-8+
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| Chemical Name |
4-[(E)-2-(5,5-dimethyl-8-phenyl-6H-naphthalen-2-yl)ethenyl]benzoic acid
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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. |
| 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 : ~16.67 mg/mL (~43.81 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 | 2.6283 mL | 13.1413 mL | 26.2826 mL | |
| 5 mM | 0.5257 mL | 2.6283 mL | 5.2565 mL | |
| 10 mM | 0.2628 mL | 1.3141 mL | 2.6283 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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