RGNCY-0125 (S-40 Tubulin inhibitor a)
S-40 is a novel, orally potent tubulin destabilisation compound. Data from crystal structure analysis revealed that S-40 occupies all three zones in the colchicine pocket with interactions distinct from other known microtubule inhibitors. S-40 overcomes paclitaxel-resistance and lacks neurotoxicity which are the limiting factors in the clinical use of paclitaxel in the treatment of cancer. S-40 inhibits the growth of cancer cell lines and patient derived organoids by inducing mitotic arrest and apoptosis. Daily oral administration of S-40 in xenograft mouse models significantly inhibited growth of non- small cell lung cancer NCI-H1299, human prostate cancer DU145 and pacltaxel-resistant A549 without apparent side effects. S-40 represents a new generation of orally effective microtubule inhibitors for cancer therapy.
Systematic Name: 3-((4-cyclopropylphenyl)sulfonamido)-4-methyl-N-(pyridin-3-ylmethyl)benzamide
Mol Wt: 421.52
Tags: Small molecules, Cancer, Apoptosis, tubulin, colchicine, RGNCY-0125, S-40, microtubule, paclitaxel