Benzoic acid, 3-fluoro-4-[[(2R)-hydroxy(5,6,7,8-tetrahydro-5,5,8,8-tetramethyl-2-naphthalenyl)acetyl]amino]-

Uses

BMS270394 is a nuclear retinoic acid receptor (RAR-γ) agonist with the EC50 values of 30 nM and 400 nM for humanRAR-γ and RAR-β, respectively[1].

Biological Activity

BMS 270394 is an agonist of retinoic acid receptor γ (RARγ; EC50 = 30 nM in a transactivation assay) and the active enantiomer of BMS 189961 .1 It is selective for RARγ over RARβ (EC50 = 400 nM) and is inactive at RARα. BMS 270394 synergizes with paclitaxel to inhibit the growth of MCF-7 breast and OVCAR-3 ovarian cancer, as well as SqCC/Y1 head and neck squamous cell carcinoma, cells.2

IC 50

RXR γ: 30 nM (EC₅₀); RXR β: 400 nM (EC₅₀)

References

1.Klaholz, B.P., Mitschler, A., Belema, M., et al.Enantiomer discrimination illustrated by high-resolution crystal structures of the human nuclear receptor hRARγProc. Natl. Acad. Sci. USA97(12)6322-6327(2000) 2.Vivat-Hannah, V., You, D., Rizzo, C., et al.Synergistic cytotoxicity exhibited by combination treatment of selective retinoid ligands with taxol (Paclitaxel)Cancer Res.61(24)8703-8711(2001)