1246532-99-9

Upstream product

• 5451-40-1 2,6 dichloropurine 
• 448-19-1 4-fluoro-2-methoxy-1-nitrobenzene 
• 39639-45-7 (2-chloro-9H-purin-6-yl)-cyclohexyl-amine 
• 89364-31-8 3-tetrahydrofuroic acid 
• 1246532-95-5 N₆-cyclohexyl-N₂-(2-methoxy-4-piperazin-1-yl-phenyl)-9H-purine-2,6-diamine 

Downstream Products

• 1246531-27-0 N₆-cyclohexyl-N₂-{2-methoxy-4-[4-(tetrahydrofuran-3-ylmethyl)piperazin-1-yl]phenyl}-9H-purine-2,6-diamine 

Relevant academic research and scientific papers

Lead optimization of purine based orally bioavailable Mps1 (TTK) inhibitors

Efforts to optimize biological activity, novelty, selectivity and oral bioavailability of Mps1 inhibitors, from a purine based lead MPI-0479605, are described in this Letter. Mps1 biochemical activity and cytotoxicity in HCT-116 cell line were improved. On-target activity confirmation via mechanism based G2/M escape assay was demonstrated. Physico-chemical and ADME properties were optimized to improve oral bioavailability in mouse.

COMPOUNDS AND THERAPEUTIC USES THEREOF

The invention relates to compounds, pharmaceutical compositions, and uses thereof, including therapeutic uses thereof, such as methods useful for treating cancer.