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Submit ReviewBexarotene
Description: Potent and selective RXR agonist
Alternative Names: LGD 1069
Chemical Name: 4-[1-(5,6,7,8-Tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)ethenyl]benzoic acid
Purity: ≥99% (HPLC)
Biological Activity for Bexarotene
Bexarotene is a potent and selective RXR agonist (EC50 values are 24, 25 and 33 nM for RXRβ, RXRγ and RXRα, respectively). Exhibits >300-fold selectivity for RXR over RAR receptors. Inhibits tumor cell invasion and migration in vitro, and inhibits metastasis and angiogenesis in mouse models. Also promotes brown adipogenic differentiation and induces brown adipogenic reprogramming from myoblasts.
Technical Data for Bexarotene
| M. Wt | 348.48 |
| Formula | C24H28O2 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 153559-49-0 |
| PubChem ID | 82146 |
| InChI Key | NAVMQTYZDKMPEU-UHFFFAOYSA-N |
| Smiles | CC(CCC(C)2C)(C)C1=C2C=C(C)C(C(C3=CC=C(C(O)=O)C=C3)=C)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Bexarotene
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 34.85 | 100 | |
| ethanol | 6.97 | 20 with gentle warming |
Preparing Stock Solutions for Bexarotene
The following data is based on the product molecular weight 348.48. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.87 mL | 14.35 mL | 28.7 mL |
| 5 mM | 0.57 mL | 2.87 mL | 5.74 mL |
| 10 mM | 0.29 mL | 1.43 mL | 2.87 mL |
| 50 mM | 0.06 mL | 0.29 mL | 0.57 mL |
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Product Datasheets for Bexarotene
References for Bexarotene
References are publications that support the biological activity of the product.
Boehm et al (1994) Synthesis and structure-activity relationships of novel retinoid X receptor-selective retinoids. J.Med.Chem. 37 2930 PMID: 8071941
Yen et al (2006) A selective retinoid X receptor agonist bexar. (LGD1069, Targretin) inhibits angiogenesis and metastasis in solid tumours. Br.J.Cancer 94 654 PMID: 16495926
Nie et al (2017) Brown adipogenic reprogramming induced by a small molecule. Cell Rep. 18 624 PMID: 28099842
If you know of a relevant reference for Bexarotene, please let us know.
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Keywords: Bexarotene, Bexarotene supplier, retinoid, X, receptors, agonists, agonism, RXR, α, β, γ, alpha, beta, gamma, potent, selective, cancer, metastasis, angiogenesis, LG1069, stem, cells, differentiation, brown, adipocytes, adipogenic, reprogramming, LGD1069, Retinoid, Receptor, Stem, Cell, Reprogramming, 5819, Tocris Bioscience
3 Citations for Bexarotene
Citations are publications that use Tocris products. Selected citations for Bexarotene include:
Hebert (2017) Effects of retinoic acid signaling on extraocular muscle myogenic precursor cells in vitro. Exp Cell Res 361 101 PMID: 29017757
McCullough et al (2018) Cell-type-specific interrogation of CeA Drd2 neurons to identify targets for pharmacological modulation of fear extinction. Transl Psychiatry 8 164 PMID: 30135420
J David et al (2022) Retinoid-X receptor agonists increase thyroid hormone competence in lower jaw remodeling of pre-metamorphic Xenopus laevis tadpoles. PLoS One 17 e0266946 PMID: 35417489
Do you know of a great paper that uses Bexarotene from Tocris? Please let us know.
Reviews for Bexarotene
Average Rating: 4 (Based on 1 Review.)
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CeA Drd2 neurons to identify targets for pharmacological modulation of fear extinction.
By
Anonymous on 02/08/2020
Assay Type: In Vivo
Species: Mouse
Cell Line/Tissue: Rosa26 fs-TRAP (B6.129S4-Gt(ROSA)26Sortm1(CAG-EGFP/Rpl10a,-birA)Wtp/J)
Bexarotene has limited solubility in water, thus it was dissolved in pure DMSO prior to injection and injected i.p. at 50 mg/kg in a volume of 0.03 ml using an insulin syringe.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Retinoid Receptors Scientific Review
Written by Alexander Moise, this review summarizes the nature of retinoid receptors, their isotype and isoform variants and modulation of retinoid signaling. Compounds available from Tocris are listed.