Benzamide, 2-[[2-[[4-(aminosulfonyl)phenyl]amino]-5-bromo-4-pyrimidinyl]amino]-6-fluoro-

TMX-3013 is a CDKs inhibitor capable of inhibiting the activity of CDK1, CDK2, CDK4, CDK5, and CDK6, with IC50 values of 0.9 nM, <0.5 nM, 24.5 nM, 0.5 nM, and 15.6 nM, respectively. TMX-3013 can be utilized for synthesizing PROTACs that feature a polyethylene glycol (PEG) linker arm and Thalidomide (HY-14658) as the CRBN-recruiting arm[1].

CDK1: 0.9 nM (IC₅₀); CDK2: <0.5 nM (IC₅₀); CDK4: 24.5 nM (IC₅₀); CDK5: 0.5 nM (IC₅₀); CDK6: 15.6 nM (IC₅₀)

[1] Teng M, et al. Development of CDK2 and CDK5 dual degrader TMX‐2172[J]. Angewandte Chemie, 2020, 132(33): 13969-13974. DOI:10.1002/anie.202004087