Bexarotene

SKU: orb1226134

Description

Bexarotene is a retinoid specifically selective for retinoid X receptors, used as an oral antineoplastic agent in the treatment of cutaneous T-cell lymphoma.(In Vitro):Bexarotene selectively binds and activates RXR subtypes with Kd=14±2 nM, 21±4 nM, and 29±7 nM for RXRα, RXRβ, and RXRγ subtypes. Bexarotene is effective in limiting the proliferation of leukemic (HL-60) cells. Bexarotene inhibits the proliferation of HL-60 cells by 37% at 1 μM. Bexarotene monotherapy of cells shows an antiproliferative effect at a high dose, and the IC50s aere 40.62±0.45 μM (PC3) and 50.20±4.10 μM (DU145). Bexarotene (20 and 40 μM) and Docetaxel (5 and 10 μM) exhibit a synergistic effect on the inhibition of PC3 and DU145 cell proliferation.Bexarotene (20 and 40 μM) represses cyclin D1 and cyclin D3 expression in PC3 and DU145 cells.\n(In Vivo):Bexarotene (1 mg/kg/day) is effective in blocking the development of behavioral deficits and dopamine neuron degeneration in a rat model of Parkinson’s disease (PD) producing significantly reduced changes in both triglycerides and T4 serum. Bexarotene is an effective preventive agent against lung tumor growth and progression. Bexarotene ((100 mg/kg by gavage) inhibits both tumor multiplicity and tumor volume in mice of all three genotypes (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt). Bexarotene reduces the progression of adenoma to adenocarcinoma by ～50% in both p53wt/wtK-rasko/wt and p53wt/wtK-raswt/wt mice.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 153559-49-0
• MW: 348
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₈O₂
• SMILES: O=C(O)C1=CC=C(C(C2=C(C)C=C3C(C)(C)CCC(C)(C)C3=C2)=C)C=C1
• Target: Retinoid Receptor
• Solubility: DMSO: 8 mg/mL (22.98 mM)

Bioactivity

• In Vivo:
  Animal model: UL53-3 mice (p53wt/wtK-raswt/wt, p53val135/wtK-raswt/wt, or p53wt/wtK-rasko/wt). Dosage: 100 mg/kg. Administration: Gavage with 18 gage of gavage-needle, 0.1 mL per mouse per day, 5 times a week, continued for 12 weeks. Result: Inhibited both tumor multiplicity and tumor volume in mice of all three genotypes.
• In Vitro:
  Cell Proliferation Assay. Cell line: The human PCa androgen-independent cell lines PC3 and DU145. Concentration: 5, 10, 20, 30, 40 μM for PC3 cells; 1, 5, 10, 20, 40 μM for DU145 cells. Incubation time: 24 and 48 hours. Result: Showed an antiproliferative effect with the IC50s were 40.62 ± 0.45 μM (PC3) and 50.20 ± 4.10 μM (DU145). Cell Viability Assay Cell line: PC3 and DU145 cells. Concentration: 20 and 40 μM. Incubation time: 24 or 48 hours. Result: Decreased cyclin D1, and cyclin E2 after 24 hours treatment. Not only decreased the expression of cyclin D1 and cyclin E2 but repressed cyclin B1 and CDK1 expression after 48 hours treatment.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LG 100069 | LGD 1069 | Ro 26-4455 | SR 11247

Quick Database Links

Gene Symbol

Retinoid Receptor