Bexarotene (Synonyms: LG 100069, LGD 1069, Ro 264455, SR 11247)

Cell lines

MJ, Hut78 and HH cell lines

Preparation method

The solubility of this compound in DMSO is > 10.4 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.1, 1 and 10 μM; 24, 48, 72 and 96 hrs

Applications

In MJ, Hut78 and HH cell lines, Bexarotene treatment for 96 hrs dose-dependently inhibited cell growth. In addition, Bexarotene increased the number of cells in the sub-G1 phase in a dose-dependent manner, which was accompanied by a loss of cells in the G1, S, and G2-M phases. However, Bexarotene did not show significant inhibition effect on cell growth and apoptosis at the dose of 0.1 to 10 μM over the period of 24 to 72 hrs in all 3 cell lines.

Animal models

MMTV-erbB2 mice

Dosage form

100 mg/kg; p.o.; q.d., 6 days per week

Applications

In MMTV-erbB2 mice, Bexarotene treatment prevented the development of hyperplasias or mammary intraepithelial neoplasia (MIN) lesions. Moreover, Bexarotene significantly inhibited mammary gland proliferation after 2- and 4- month treatments. The immunohistochemical results showed that less than 1% of mammary epithelial cells in the Bexarotene treatment group showed positive caspase 3 staining, indicating that the cancer preventive effect of Bexarotene was not attributed to the induction of apoptosis.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Zhang C, Hazarika P, Ni X, Weidner DA, Duvic M. Induction of apoptosis by bexarotene in cutaneous T-cell lymphoma cells: relevance to mechanism of therapeutic action. Clin Cancer Res. 2002 May;8(5):1234-40.

[2]. Li Y, Zhang Y, Hill J, Kim HT, Shen Q, Bissonnette RP, Lamph WW, Brown PH. The rexinoid, bexarotene, prevents the development of premalignant lesions in MMTV-erbB2 mice. Br J Cancer. 2008 Apr 22;98(8):1380-8.