TMX-2172 is a potent, selective CDK2 and CDK5 dual PROTAC degrader with IC50 of 6.5 nM and 6.8 nM for CDK2/cyclin A and CDK5/p25, respectively.
TMX-2172 shows high degradation selectivity for CDK2 and CDK5 over other cell cycle CDKs (CDK1, CDK4, and CDK6) and transcriptional CDKs (CDK7 and CDK9).
TMX-2172 exhibits antiproliferative activity against OVCAR8 with IC50 of 33.1 nM, an ovarian cancer cell line that overexpresses CCNE1 (a well-established activator of CDK2).
TMX-2172 exhibits an IC50 of 46.9 nM in cellular CRBN engagement assays.
TMX-2172 induced CDK2 degradation at a concentration of 250 nM in Jurkat cells with no effect against other cell cycle CDKs.
