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Abemaciclib
    Publish time 2024-09-26 20:03    

CAS NO.: 1231929-97-7

Abemaciclib

Basic Information

  • Chinese Name: 阿贝西利

  • English Name: Abemaciclib

  • CAS Number: 1231929-97-7

  • Molecular Formula: The specific molecular formula may vary depending on the source or product, but it is related to the chemical structure of Abemaciclib.

  • Molecular Weight: Similarly, the exact molecular weight will also vary based on the chemical structure.

Pharmacological Action

  • Abemaciclib inhibits the activity of CDK4 and CDK6 with IC50 values of 2 nM and 10 nM, respectively, demonstrating potent inhibition of these two kinases.

  • By inhibiting CDK4/6, Abemaciclib prevents the transition of the cell cycle from the G1 phase to the S phase, thereby inhibiting tumor cell proliferation.

  • In vitro experiments have shown that Abemaciclib reduces the viability of various tumor cells, including head and neck squamous cell carcinoma (HNSCC) cells, and inhibits Akt and ERK signaling pathways without affecting mTOR activation.

  • In vivo experiments have demonstrated that Abemaciclib in combination with RAD001 exhibits synergistic antitumor effects in HNSCC xenograft tumor models, and Abemaciclib alone significantly inhibits tumor growth in A375 xenograft models.

Clinical Applications

  • Abemaciclib has been approved for the treatment of certain types of breast cancer, specifically hormone receptor-positive, HER2-negative advanced or metastatic breast cancer, in patients who are no longer sensitive to endocrine therapy or have received prior chemotherapy.

  • In clinical studies, Abemaciclib has shown potential to prolong progression-free survival (PFS) and improve quality of life for patients.