Fluorobexarotene Inhibitor

Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene. Fluorobexarotene is a potent retinoid-X-receptor (RXR) agonist, with a Ki value of 12nM and an EC50 value of 43nM for RXRalpha receptor. Fluorobexarotene possesses an apparent RXR binding affinity that is 75% greater than Bexarotene.

Wagner CE, et al. Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene). J Med Chem. 2009 Oct 8;52(19):5950-66.
Wagner CE, et al. Modeling, synthesis and biological evaluation of potential retinoid X receptor (RXR) selective agonists: novel analogues of 4-[1-(3,5,5,8,8-pentamethyl-5,6,7,8-tetrahydro-2-naphthyl)ethynyl]benzoic acid (bexarotene). J Med Chem. 2009 Oct 8;52(19):5950-66.

Small volumes of Fluorobexarotene, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

MBS5753134 is an inhibitor targeting Fluorobexarotene.