LY335979 is a cyclopropyldibenzosuberane-based P-glycoprotein modulator for which Pgp has an affinity at 59 nM. At 100 nM, LY335979 sensitizes a number of Pgp-expressing resistant cell lines to oncolytics. [1] LY335979 does not affect multidrug resistance-associated protein 1 or 2, and has a lower affinity for CYP3A than Pgp.

In primary acute myeloid leukemia blasts with active Pgp, LY335979 completely or partially resotred drug sensitivity in cell lines tested and enhanced the cytotoxicity of anthracyclines such as daunorubicin, idarubicin, mitoxantrone; additionally, LY335979 was found to be more potent than cyclosporine A in cells with highly-active Pgp. [2]

In coadministration studies with popular anticancer agents such as Doxorubicin and etoposide, LY335979 was shown to have no negative effect on drug pharmacokinetics. [3]

Technical information:

Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder at 4^oC desiccated, or store DMSO solution at -20^oC.

Reference:

Other Information:

Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.