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CDK4/6 degrader BTX-9341

An orally bioavailable bifunctional degrader of cyclin-dependent kinase (CDK) types 4 (CDK4) and 6 (CDK6), with potential antineoplastic activity. Upon oral administration, CDK4/6 degrader BTX-9341 targets and binds to CDK4 and CDK6, as well as cereblon (CRBN), a component of the CRL4-CRBN E3 ubiquitin ligase complex that directs proteins for destruction. This leads to ubiquitination and induces proteasome-mediated degradation of CDK4 and CDK6, thereby inhibiting the phosphorylation of retinoblastoma protein (Rb) early in the G1 phase, preventing CDK-mediated G1-S-phase transition and leading to cell cycle arrest. This suppresses DNA replication and decreases tumor cell proliferation. CDK4 and 6 are serine/threonine kinases that are upregulated in many tumor cell types and play a key role in the regulation of both cell cycle progression from the G1-phase into the S-phase and tumor cell proliferation. BTX-9341 is able to penetrate through the blood-brain barrier (BBB).
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Code name:BTX 9341
BTX-9341
BTX9341
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