2089211-45-8

Paclitaxel octadecanedioate is a prodrug form of paclitaxel that is comprised of paclitaxel conjugated to 1,18-octadecanedioic acid.¹ Unlike paclitaxel, it does not promote tubulin polymerization in vitro when used at a concentration of 10 μM. A 5:1 mixture of paclitaxel octadecanedioate:human serum albumin (HSA) is cytotoxic to HT-1080, PANC-1, and HT-29 cells (IC₅₀s = 12, 2.48, and 8.62 nM, respectively). This mixture reduces tumor growth and increases survival in an HT-1080 mouse xenograft model in a dose-dependent manner.

Paclitaxel octadecanedioate (compound PTX-FA18) is comprised of Paclitaxel (HY-B0015) conjugated to 1,18-octadecanedioic acid (HY-W005178). Paclitaxel octadecanedioate mixed with human serum albumin (HAS) is cytotoxic to HT-1080, PANC-1, HT-29 and Hela cells (IC50s = 12, 2.48, 8.62, and 64.42 nM, respectively)[1].

1. Callmann, C.E., Leguyader, C.L.M., Burton, S.T., et al. Antitumor activity of 1,18-octadecanedioic acid-paclitaxel complexed with human serum albumin J. Am. Chem. Soc. 141(30),11765-11769(2019).