| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
|
||
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| Other Sizes |
|
Purity: ≥98%
Bexarotene (Ro26-445; LGD-1069; SR-11247; Ro-26 445; Targretin Ro 26-44) is a synthetic retinoid analog and selective agonist of RXR-retinoid X receptors with potential anticancer chemopreventive, teratogenic and embryotoxic properties. Bexarotene has been approved as an oral anticancer agent for the treatment of cutaneous T-cell lymphoma. Bexarotene selectively binds to and activates retinoid X receptors, thereby inducing changes in gene expression that lead to cell differentiation, decreased cell proliferation, apoptosis of some cancer cell types, and tumor regression.
| ln Vitro |
Bexarotene preferentially binds and activates RXR isoforms with Kd=14±2 nM, 21±4 nM and 29±7 nM for RXRα, RXRβ and RXRγ isoforms [1]. Bexarotene efficiently reduces the proliferation of leukemia (HL-60) cells. Bexarotene inhibits HL-60 cell proliferation by 37% at 1 μM [1]. Bexarotene treated cells as a single agent displayed anti-proliferative effects at high doses, with IC50s of 40.62±0.45 μM (PC3) and 50.20±4.10 μM (DU145) [2]. Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) show synergistic effects on the suppression of PC3 and DU145 cell growth [2]. Bexarotene (20 and 40 μM) suppresses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells [2].
|
|---|---|
| ln Vivo |
In a rat model of Parkinson's disease (PD), bexarotene (1 mg/kg/day) effectively prevents the development of behavioral deficits and dopamine neuron degeneration, thereby significantly reducing changes in serum T4 and triglycerides [1]. One medication that works well at stopping the development and spread of lung tumors is bexarotene. In mice of all three genotypes (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt), bexarotene (100?mg/kg by gavage) inhibits tumor diversity and tumor volume. Bexarotene decreased the progression of adenoma to adenocarcinoma in p53wt/wtK-rasko/wt by about 50%. and mice that were p53wt/wtK-raswt/wt [3].
|
| Cell Assay |
Cell Proliferation Assay[2]
Cell Types: The human PCa androgen-independent cell lines PC3 and DU145 Tested Concentrations: 5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells. Incubation Duration: 24 and 48 hrs (hours) Experimental Results: demonstrated an antiproliferative effect with the IC50s were 40.62±0.45 µM (PC3) and 50.20±4.10 µM (DU145). Cell Viability Assay[2] Cell Types: PC3 and DU145 cells Tested Concentrations: 20 and 40 µM Incubation Duration: 24 or 48 hrs (hours) Experimental Results: diminished cyclin D1, and cyclin E2 after 24 hrs (hours) treatment. Not only diminished the expression of cyclin D1 and cyclin E2 but repressed cyclin B1 and CDK1 expression after 48 hrs (hours) treatment. |
| Animal Protocol |
Animal/Disease Models: UL53-3 mice (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt)[3]
Doses: 100 mg/kg Route of Administration: Gavage with 18 gage of gavage -needle, 0.1 mL per mouse per day, 5 times a week, continued for 12 weeks Experimental Results: Inhibited both tumor multiplicity and tumor volume in mice of all three genotypes. |
| References |
[1]. Nathalia Rodrigues de Almeida, et al. A review of the molecular design and biological activities of RXR agonists. Med Res Rev. 2019 Jul;39(4):1372-1397.
[2]. Danyang Shen, et al. Synergistic effect of a retinoid X receptor-selective ligand bexarotene and docetaxel in prostate cancer. Onco Targets Ther. 2019 Sep 24;12:7877-7886. [3]. Y Wang, et al. Prevention of lung cancer progression by bexarotene in mouse models. Oncogene. 2006 Mar 2;25(9):1320-9. |
| Molecular Formula |
C24H28O2
|
|---|---|
| Molecular Weight |
348
|
| CAS # |
153559-49-0
|
| Related CAS # |
Bexarotene-d4;2182068-00-2
|
| SMILES |
O=C(O)C1=CC=C(C(C2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2)=C)C=C1
|
| Synonyms |
LGD1069; LGD 1069; LG 100069; Ro26-445; LGD-1069; SR-11247; Ro 26 445; Targretin Ro 26-445; SR 11247; SR11247; 3-methyl TTNEB. Bexarotene; US trade name: Targretin.
|
| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| 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) |
|
|---|
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8736 mL | 14.3678 mL | 28.7356 mL | |
| 5 mM | 0.5747 mL | 2.8736 mL | 5.7471 mL | |
| 10 mM | 0.2874 mL | 1.4368 mL | 2.8736 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
NMR
