Bexarotene (Synonyms: LG 100069, LGD 1069, Ro 264455, SR 11247) |
| رقم الكتالوجGC10037 |
Bexarotene (LGD1069) هو ناهض عالي التقارب ومستقبلات ريتينويد X انتقائية (RXR) مع EC50s من 33 ، 24 ، 25 نانومتر لـ RXRα و RXRβ و RXRγ ، على التوالييُظهر Bexarotene تقاربًا محدودًا لمستقبلات RAR (EC50> 10000 نانومتر)يمكن استخدام Bexarotene في البحث عن سرطان الغدد الليمفاوية T-cell الجلدي
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 153559-49-0
Sample solution is provided at 25 µL, 10mM.
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Bexarotene is a selective activator of retinoid X receptor (RXR), with EC50 values of 0.028, 0.025, and 0.020µM for RXRα, RXRβ and RXRγ, respectively[1]. Bexarotene can increase arylsulfatase A (ARSA) activity with an EC50 value of 3.4μM[2]. Bexarotene can be used as a model compound to develop a series of new derivatives and to evaluate the cytotoxicity of Bexarotene in glioma cells[3].
In vitro, Bexarotene treatment for 48 hours showed an anti-proliferative effect with IC50 values of 40.62±0.45µM for PC3 cells, and 50.20±4.10µM for DU145 cells[4]. Treatment of ovarian cancer cells with 10µM Bexarotene for 24h significantly inhibited cell viability, reduced cell cyclin-related protein expression, and induced cell cycle arrest and pyroptosis[5]. Bexarotene treatment (75μM; 24 hours) can reduce the levels of NF-κB and TAS in C6 cells, and increase the levels of PPARγ and 8-OHdG, stimulating oxidative stress in the cells[6].
In vivo, Bezafibrate treatment via oral administration (0.3mg/kg/day) for 28 days alleviated the progression of motor dysfunction in the Parkinson's disease rat models, improved cognitive impairment, and reduced head twitching[7]. Bexarotene treatment (100mg/kg/day; p.o.) for 30 days significantly reduced soluble β-amyloid and astrogliosis, accompanied by enhanced cognitive improvement in murine models of Alzheimer’s disease (AD)[8].
References:
[1] Boehm M F, Zhang L, Zhi L, et al. Design and synthesis of potent retinoid X receptor selective ligands that induce apoptosis in leukemia cells[J]. Journal of medicinal chemistry, 1995, 38(16): 3146-3155.
[2] Schlotawa L, Tyka K, Kettwig M, et al. Drug screening identifies tazarotene and bexarotene as therapeutic agents in multiple sulfatase deficiency[J]. EMBO molecular medicine, 2023, 15(3): e14837.
[3] Gretskaya N M, Gamisonia A M, Dudina P V, et al. Novel bexarotene derivatives: Synthesis and cytotoxicity evaluation for glioma cells in 2D and 3D in vitro models[J]. European Journal of Pharmacology, 2020, 883: 173346.
[4] Shen D, Wang H, Zheng Q, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer[J]. OncoTargets and therapy, 2019: 7877-7886.
[5] Kobayashi T, Mitsuhashi A, Hongying P, et al. Bexarotene-induced cell death in ovarian cancer cells through Caspase-4-gasdermin E mediated pyroptosis[J]. Scientific reports, 2022, 12(1): 11123.
[6] Hacioglu C, Kar F, Kacar S, et al. Bexarotene inhibits cell proliferation by inducing oxidative stress, DNA damage and apoptosis via PPARγ/NF-κB signaling pathway in C6 glioma cells[J]. Medical Oncology, 2021, 38(3): 1-11.
[7] McFarland K, Spalding T A, Hubbard D, et al. Low dose bexarotene treatment rescues dopamine neurons and restores behavioral function in models of Parkinson’s disease[J]. ACS chemical neuroscience, 2013, 4(11): 1430-1438.
[8] Muñoz-Cabrera J M, Sandoval-Hernández A G, Niño A, et al. Bexarotene therapy ameliorates behavioral deficits and induces functional and molecular changes in very-old Triple Transgenic Mice model of Alzheimer´ s disease[J]. PLoS One, 2019, 14(10): e0223578.
| Cell experiment [1]: | |
Cell lines | PC3 cells |
Preparation Method | PC3 cells were cultured in RPMI-1640 medium supplemented with 10% fetal bovine serum and penicillin-streptomycin. Cells were cultured at 37°C in a 5% CO2 environment. Cells (6×103/well) were seeded in 96-well plates and allowed to adhere overnight. Different concentrations of Bexarotene (0, 5, 10, 20, 30, and 40µM) were added to the cells. After 48 hours of incubation, a tenth volume of MTT (5mg/mL, dissolved in PBS buffer) was added to each well, and the culture plates were incubated for another 2 hours, the absorbance value at 550nm was measured. |
Reaction Conditions | 0, 5, 10, 20, 30, and 40µM; 48h |
Applications | Bexarotene significantly inhibited the proliferation of PC3 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Triple-transgenic Alzheimer’s disease (AD) mice |
Preparation Method | Female and male 24-month-old triple transgenic AD (3×TgAD) mice were housed in polycarbonate cages in a soundproof room, in groups of five, with free access to water and food throughout the experiment, and housed under controlled environmental conditions, with a 12-hour light/dark cycle (light on from 07:00 to 19:00), room temperature of 20±1°C, and relative humidity of 50±10%. All mice received 100mg/kg/day Bexarotene or polyethylene glycol 400 (30% v/v) and polysorbate-20 (1% v/v in distilled water) daily by oral gavage for 30 days. Brain tissue samples from mice were collected for immunofluorescence analysis and Western blot analysis. |
Dosage form | 100mg/kg/day for 30 days; p.o. |
Applications | Bexarotene treatment significantly reduced soluble β-amyloid and astrogliosis, accompanied by enhanced ApoE protein expression in 3×TgAD mice. |
References: | |
| Cas No. | 153559-49-0 | SDF | |
| المرادفات | LG 100069, LGD 1069, Ro 264455, SR 11247 | ||
| Chemical Name | 4-[1-(3,5,5,8,8-pentamethyl-6,7-dihydronaphthalen-2-yl)ethenyl]benzoic acid | ||
| Canonical SMILES | CC1=CC2=C(C=C1C(=C)C3=CC=C(C=C3)C(=O)O)C(CCC2(C)C)(C)C | ||
| Formula | C24H28O2 | M.Wt | 348 |
| الذوبان | ≥ 10.35mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.8736 mL | 14.3678 mL | 28.7356 mL |
| 5 mM | 574.7 μL | 2.8736 mL | 5.7471 mL |
| 10 mM | 287.4 μL | 1.4368 mL | 2.8736 mL |
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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