365565-02-2

PGP-4008 is a selective inhibitor of P-glycoprotein (P-gp) that does not affect the activity of multidrug resistance-related protein 1 (MRP1). It is effective in vitro and, when delivered intraperitoneally, in vivo, inhibiting tumor growth when given with doxorubicin . PGP-4008 also enhances the ability of docetaxel to inhibit growth and drive apoptosis in ovarian cancer cells.

PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin[1].

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[1] Brian D Lee, et al. Synthesis and evaluation of dihydropyrroloquinolines that selectively antagonize P-glycoprotein. J Med Chem. 2004 Mar 11;47(6):1413-22. DOI:10.1021/jm0303204