TMX-2172

• Target:

  CDK|||PROTACs

• Related Pathways:

  PROTAC|||Cell Cycle/Checkpoint

• Bioactivity:

  TMX-2172 is a heterobifunctional CDK2 degrader, selectively degrading CDK2 and CDK5, with minimal effects on CDK1, transcriptional CDKs (CDK7 and CDK9), and cell cycle CDKs (CDK4 and CDK6) . In ovarian cancer cells (OVCAR8), its anti-proliferative activity is dependent on CDK2 degradation and is linked to high expression of cyclin E1 (CCNE1), which acts as a regulatory subunit of CDK2. As a lead compound for further development, TMX-2172 demonstrates that CDK2 degradation could be a potentially effective strategy for treating ovarian and other cancers with elevated CCNE1 expression.

• Smiles:

  O=C (N) C=1C (F) =CC=CC1NC2=NC (=NC=C2Br) NC3=CC=C (C=C3C) S (=O) (=O) NCCOCCOCCOCCOCCNC4=CC=CC=5C (=O) N (C (=O) C45) C6C (=O) NC (=O) CC6

• Molecular Formula:

  C41H45BrFN9O11S

• Molecular Weight:

  970.82

• Shipping Conditions:

  Cool pack

• Storage Temperature:

  -20°C

• CAS Number:

  2488892-09-5