SP-1-39

SP-1-39 is a small molecule tubulin inhibitor that targets the colchicine binding site (CBSI). Developed by researchers at the University of Tennessee Health Science Center, it is a pyrimidine dihydroquinoxalinone derivative designed to improve upon the potency and pharmacokinetic properties of earlier CBSIs like SB-216. SP-1-39 is highly brain-penetrable and has shown significant preclinical efficacy in models of breast cancer brain metastasis (BCBM), triple-negative breast cancer (TNBC), head and neck squamous cell carcinoma (HNSCC), and castration-resistant prostate cancer. It works by disrupting microtubule dynamics, leading to G2/M phase cell cycle arrest and apoptosis. Notably, it maintains activity in taxane-refractory (paclitaxel-resistant) tumors, potentially overcoming common resistance mechanisms like P-glycoprotein efflux.

Other names

7-Methoxy-4-(2-(methylamino)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)-3,4-dihydroquinoxalin-2(1H)-one