BLX-3030

BLX-3030 is an orally available, potent, and selective small molecule inhibitor of cyclin-dependent kinase 9 (CDK9), developed by Biolexis Therapeutics. It acts by reversibly binding to CDK9 and competitively blocking the ATP-binding site, with an IC50 of less than 5 nM. This inhibition leads to reduced phosphorylation of CDK9 and downstream targets such as C-MYC, N-MYC, Mcl-1, RNA polymerase II (Ser-2), and androgen receptor (Ser-81). The drug has demonstrated significant antitumor activity in preclinical models of MYC-driven cancers—particularly prostate cancer—showing tumor growth inhibition greater than 70% in multiple mouse xenograft models. BLX-3030 has also shown efficacy in pancreatic cancer and other solid tumors during preclinical studies. Its pharmacokinetic profile includes good oral bioavailability (28–82% in rodents/canines) and a half-life exceeding three hours[1][2][5].

Other names

BLX 3030BLX3030BLX-3030